Category: 52537-00-5

On June 13, 2013, Yang, Shyh-Ming; Kuo, Gee-Hong; Gaul, Micheal D.; Rano, Thomas A. published a patent.Recommanded Product: 52537-00-5 The title of the patent was Preparation of substituted piperidinyl-pyridazinyl derivatives as SCD1 inhibitors. And the patent contained the following:

The title compounds I [R1 = P1, P2, P3, etc.; wherein m = 0-3; R2 = halo, C1-4 alkyl, C1-4 alkoxy, etc.; R3 = Q1, Q2, Q3, etc.; wherein R4 = H, halo, C1-4 alkyl, etc.] or pharmaceutically acceptable salts thereof were prepared Compounds I are useful as Stearoyl-CoA desaturase 1 (SCD1) inhibitors for treatment of obesity, type 2 diabetes and other related metabolic disorders. For example, compound II was prepared in a multi-step synthesis and displayed IC50 of 0.12 μM against SCD1 in A431 cells. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 52537-00-5

The Article related to piperidinyl pyridazinyl derivative preparation scd1 inhibitor, obesity type 2 diabetes treatment piperidinyl pyridazinyl derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Recommanded Product: 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 11, 2015, Yang, Shyh-Ming; Kuo, Gee-Hong; Gaul, Micheal D.; Rano, Thomas A. published a patent.COA of Formula: C8H8ClN The title of the patent was Substituted piperidinyl-pyridazinyl derivatives useful as scd 1 inhibitors. And the patent contained the following:

The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).COA of Formula: C8H8ClN

The Article related to piperidinyl pyridazinyl derivative preparation scd1 inhibitor, obesity type 2 diabetes treatment piperidinyl pyridazinyl derivative preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.COA of Formula: C8H8ClN

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On May 27, 2021, Jing, Peng; Guo, Qiang; Dou, Fei; Wan, Zehong; Hu, Zhijing published a patent.Name: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Fused heterocyclic derivative and application. And the patent contained the following:

The invention disclosed a kind of fused heterocyclic derivative, its preparation method and application for treating neuropsychiatric diseases. The claimed compound is shown in structure I (Z = O or S C2-8 chain or halo substituted C2-8 chain; A = II; R = heteroaryl; Q = N or CH; Y = O or S; R1,R2,R3 = H, halo, C1-6 alkyl, etc.; n1 = 1-3 integers). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used for treating neuropsychiatric diseases such as schizophrenia, depression, anxiety, sleep disorders, neurodegenerative diseases, bipolar disorder, post-traumatic stress syndrome, addiction disorders, abstinence syndrome, or attention deficit. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Name: 6-Chloro-2,3-dihydro-1H-indole

The Article related to fused heterocyclic derivative preparation neuropsychiatric disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Name: 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 28, 1997, Arnold, Daniel Lee; Moyer, Mikel Paul; Sobolov-Jaynes, Susan Beth published a patent.SDS of cas: 52537-00-5 The title of the patent was Heterocyclic ring-fused pyrimidine derivatives, their intermediates and pharmaceutical compositions containing them. And the patent contained the following:

The invention refers to fused pyrimidines I [Y, together with the attached carbon atoms, form a 5- or 6-membered substituted aromatic ring, optionally containing 1-3 nitrogen atoms, and in addition optionally containing O or S; Z = NR1R2, Z’; R1 = H; R2 = Ph; R5 = various substituents, inc, heterocycles; R6 = OH, NH2, substituted amino, (un)substituted alkyl; n = 0, 1, 2; m = 1, 2, 3; dashed line = single or double bond], their stereoisomers and pharmaceutical medically acceptable salts and prodrugs. Thus, N-(3-ethynylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride II·HCl was prepared from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine via amination with (3-aminophenyl)acetylene in pyridine followed by treatment with HCl in MeOH. These compounds inhibit the receptor tyrosine kinase enzymes and thus, they are able to selectively prevent the multiplication of breast cancer cells (no data). On the basis of this, they can be used to treat different hyperproliferative diseases, such as cancer of the lung, bladder, stomach, pancreas, liver, kidney, large intestine and rectum, as well as gynecol. cancers. In addition, they are suitable for the treatment of other non-cancerous hyperproliferative diseases, such as psoriasis, or non-malignant prostate hypertrophy. The invention also includes the pharmaceutical products that contain effectives doses of the general formula compounds as their active component, and the new intermediate products, which can be applied during the synthesis of the compounds according to the invention. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).SDS of cas: 52537-00-5

The Article related to fused pyrimidine derivative preparation antiproliferative, psoriasis medicinal fused pyrimidine derivative, prostate hypertrophy medicinal fused pyrimidine derivative, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

De, Pinaki Bhusan; Banerjee, Sonbidya; Pradhan, Sourav; Punniyamurthy, Tharmalingam published an article in 2018, the title of the article was Ru(II)-Catalyzed C7-acyloxylation of indolines with carboxylic acids.SDS of cas: 52537-00-5 And the article contains the following content:

A method for the synthesis of 1-(pyrimidin-2-yl)indolin-7-yl-carboxylate derivative I [R = Ph, 2-thienyl, 1-naphthyl, etc.; R1 = H, 2-Me, 3-Me; R2 = H, 6-Cl, 4-Br, etc.] via ruthenium(II)-catalyzed site-selective C7-acyloxylation of indolines with carboxylic acids was presented. The substrate scope and functional group tolerance were important practical features. The kinetic isotope studies suggested that C-H bond activation might be the rate-determining step. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).SDS of cas: 52537-00-5

The Article related to pyrimidinyl indolinyl carboxylate regioselective preparation, pyrimidyl indoline carboxylic acid acyloxylation ruthenium catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 7, 2021, Zhong, Wenge; Zhu, Xiaotian; Feng, Song; Wu, Lei; Huang, Wei; Liu, Hao; Liu, Rongqiang; Wen, Kate Xin; Zhou, Hua published a patent.Safety of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of substituted tetrahydroisoquinolinylaminopyridines and pyrrolopyridinylphenyldialkyl phosphine and their analogs as HPK1 inhibitors for treating cancers. And the patent contained the following:

The invention is related to the preparation of compounds I [X = CR2R3, NR3; A = CR2, N; R = 8-10 membered bicyclic N-containing heteroaryl or 8-10 membered bicyclic N-containing heterocyclyl optionally substituted with oxo, wherein the heteroaryl or heterocyclyl represented by R has 1 to 3 heteroatoms selected from N, O, and S, and is further optionally substituted, and wherein R is either connected with the pyrimidine ring via a nitrogen ring atom or R = (un)substituted quinolin-4-yl, indol-1-yl, isoquinolin-1-yl, etc.; R1 = H, D, halo,, OH, CN, NH2, NO2, etc.; or R and R1 together with the carbon atoms to which they are attached, form a ring selected from II, III, IV, etc.; Rb = independently at each occurrence H, D, COOH, etc.; Rc = independently Ph, 5-6 membered monocyclic heterocyclyl having 1-3 heteroatoms selected from N and O; 5-6 membered monocyclic heteroaryl having 1-3 heteroatoms selected from N and O; wherein the Ph, heterocyclyl, or heteroaryl represented by R is optionally substituted with one to three substituents independently selected from the group consisting of halogen, OH, CN, etc.; m = 0-3; Y = (CH2)p; p = 1-3; Z = (CH2)q; q = 1-3 and p+q ≤4], their pharmaceutically acceptable salts and stereoisomers as hematopoietic progenitor kinase 1 (HPK1)inhibitors for treating cancers. The invention is also related to the preparation of compounds V [A1 = CR’, N; X = P(O)R3R4; R’ = H, D, halo, CN, NO2, etc.; R1′ = independently at each occurrence H, D, OH, (un)substituted alk(en/yn)yl, etc.; R2′ = independently at each occurrence H, NO2, alkoxycarbonyl, etc.; m, n = independently 0-2] as HPK1 inhibitors for treating cancers. Thus, reaction of (1H-indol-3-yl)dimethylphosphine oxide (preparation given) with [1-(2,5-dichloropyrimidin-4-yl)-1H-indol-3-yl]dimethylphosphine oxide and treatment of the resulting [1-[5-chloro-2-[(6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl)amino]pyrimidin-4-yl]-1H-indol-3-yl]dimethylphosphine oxide with 6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-amine gave VI. VI inhibited HPK1 and JAK3 kinases with IC50 of ≤100μ=nM and > 1μM, resepctively. Certain HPK1 inhibitors I and V are selective against one or more kinases selected from: Lck, ZAP70, JAK3, PKC-theta, TBK1, and MAP4K3. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Safety of 6-Chloro-2,3-dihydro-1H-indole

The Article related to tetrahydroisoquinolinylaminopyrimidine pyrrolopyridinylphenyldialkyl phosphine preparation hpk1 inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Pei-Long; Li, Yan; Ma, Lan; Luo, Chen-Guang; Wang, Zhen-Yu; Lan, Quan; Wang, Xi-Sheng published an article in 2016, the title of the article was Palladium-Catalyzed C-7 Selective C-H Carbonylation of Indolines for Expedient Synthesis of Pyrroloquinazolinediones.Application of 52537-00-5 And the article contains the following content:

A novel palladium-catalyzed C-7 selective C-H carbonylation of indolines with carbon monoxide for an expedient synthesis of pyrroloquinazolinediones, a structural motif with great potential in biol. active compounds, has been developed. Oxidation of the pyrroloquinazolinedione with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) could easily afford the corresponding indole-based derivative in excellent yield. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to pyrroloquinazolinedione preparation, carbon monoxide carbonylation indoline palladium catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On November 10, 2016, Lan, Jiong; Zhou, Fusheng; Zhao, Jinzhu; Xu, Feng; Shi, Xia; Xie, Jing; Xu, Hui; Wang, Lixiao published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Bicyclic substituted benzene sulfonamide derivatives as voltage-gated sodium channel inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to bicyclic substituted benzene sulfonamide derivatives of formula I, and the preparation method and pharmaceutical use as voltage-gated sodium channel inhibitors in the treatment of diseases thereof. In particular, disclosed in the present invention are the compounds of formula I or their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof, and the preparation method and use thereof. Compounds of formula I wherein R1-R4 are independently H, OH, CN, NO2, halo, NH2 and derivatives, C1-20 alkyl, C3-20 cycloalkly, etc.; R5 is 5- to 6-membered heteroaryl, -CO-C1-20 alkyl, C3-20 cycloalkyl; L1 and L2 are independently a bond, -(CH2)1-3, etc.; dotted double bond is either a single bond or a double bond; X is a bond, NH and derivatives, O, S; Z1 is (un)substituted CH2, O, -CO-, (un)substituted -CH=, -N=, etc.; Z2 is -CO-, (un)substituted CH2, -NH- and derivatives, =N-, (un)substituted =CH-, O, etc.; Z3 is NH and derivatives, CH2, (un)substituted -CH=, etc.; Z4 is a bond, NH and derivatives, CH2, (un)substituted =CH-, =N-, etc.; ring A is (un)substituted 5- to 6-membered (hetero)aryl, etc.; and their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs as voltage-gated sodium channel inhibitors useful in the treatment of diseases thereof, are claimed. Compounds of formula I were prepared by using condensation as the key step. All the invention compounds were evaluated for their voltage-gated sodium channel inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

The Article related to benzenesulfonamide preparation voltage gated sodium channel inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On March 27, 2008, Chen, Li; Zhang, Jing; Zhang, Zhuming; Yang, Song published a patent.Formula: C8H8ClN The title of the patent was Oxindole derivatives as anticancer agents and their preparation, pharmaceutical compositions and use in the treatment of proliferative and oncological diseases. And the patent contained the following:

There is provided compounds of the formula I, which exhibited activity as anticancer agents. Compounds of formula I wherein X is H, halo, CN, lower alkyl, lower alkenyl, lower alkynyl, etc.; V is H and halo; Y is (un)substituted lower alkylamino, (un)substituted (hetero)arylamino, (un)substituted dialkylamino, (un)substituted lower alkoxy, (un)substituted (hetero)aryloxy, etc.; W is O, N and a single bond; n is 1 – 3; R6 is (un)substituted heteroaryl; and their pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by condensation of 6-chlorooxindole with 3-chlorobenzaldehyde; the resulting 3-(3-chlorobenzylidene)-6-chlorooxindole underwent hydride reduction to give 3-(3-chlorobenzyl)-6-chlorooxindole, which underwent bromination to give 3-bromo-3-(3-chlorobenzyl)-6-chlorooxindole, which underwent amination with 4-propoxyaniline to give compound II. All the invention compounds were evaluated for their anticancer activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Formula: C8H8ClN

The Article related to oxindole derivative preparation anticancer treatment proliferative oncol disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C8H8ClN

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On December 8, 1982, there was a patent about fungicides.Category: indole-building-block The title of the patent was 1-(α-Chloroacetyl)-6-substituted indolines. And the patent contained the following:

Title indolines I [R = COCH2Cl (II), COCH2NO2] were prepared by acylating I (R = H) in the presence of bases. Thus, 14.7 g ClCH2COCl was added to a mixture of 20 g I (R = H) and 14.4 g Et3N in C6H6 with cooling and the whole stirred 30 min with cooling and 2 h at 30-40° to give 74.8% II. II showed fungicidal activity at 1000 ppm. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Category: indole-building-block

The Article related to indoline chloro fungicide preparation, chloroindoline acyl fungicide preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles