Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.25235-85-2,4-Chloroindole,as a common compound, the synthetic route is as follows.

General procedure: POCl3 (13.09 g, 85.36 mmol) was slowly added dropwise to DMF(10 mL) under ice bath. The mixture was stirred at ice bath for30 min. Then, DMF (6.24 g, 85.36 mmol) solution of indole (5 g,42.68 mmol) was added dropwise to the reaction system. Keepingthe reaction at room temperature for 3 h, ice water and 10% NaOHaq. were added into the reaction system to pH of 7-8 and continue to stir to a lot of white solid precipitation. The solid was recrystallizedfrom ethyl acetate and petroleum ether to obtain compound3 in yields of 97.6%., 25235-85-2

Big data shows that 25235-85-2 is playing an increasingly important role.

Reference£º
Article; Liu, Hong-Min; Suo, Feng-Zhi; Li, Xiao-Bo; You, Ying-Hua; Lv, Chun-Tao; Zheng, Chen-Xing; Zhang, Guo-Chen; Liu, Yue-Jiao; Kang, Wen-Ting; Zheng, Yi-Chao; Xu, Hai-Wei; European Journal of Medicinal Chemistry; vol. 175; (2019); p. 357 – 372;,
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

15861-24-2, Indole-5-carbonitrile is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 69: l-(Benzenesulfonyl)indole-5-carbonitrile; [812] To 30OmL of anhydrous tetrahydrofuran was dissolved sodium hydride (23.4g, 537mmol) at O0C. lH-indole-5-carbonitrile (25.43g, 179mmol) was dissolved in 10OmL of anhydrous tetrahydrofuran, which was then slowly added in drops at O0C. The mixture was stirred for 30 min. Benzenesulfonyl chloride (63.2g, 358mmol) was dissolved in 10OmL of anhydrous tetrahydrofuran, which was then slowly added in drops at O0C. The mixture was slowly warmed to room temperature while stirring for 15 h. After completion of the reaction, ethyl acetate was added. The mixture was washed with IN hydrochloric acid. The organic layer was concentrated under reduced pressure, and the resulting solid was washed with ethanol and dried to give 45.84g (157mmol, Yield 86%) of the title compound.[813] NMR 1H-NMR(CDCl3) delta 8.09(1H, d), 7.90(3H, m), 7.7O(1H, d), 7.55-7.62(2H, m), 7.49(2H, t), 6.73(1H, d)[814] Mass(EI): 283(M++1), 15861-24-2

15861-24-2 Indole-5-carbonitrile 27513, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; LG LIFE SCIENCES LTD.; CHOI, Sung Pil; KIM, Geun Tae; SONG, Jeong Uk; KIM, Tae Hun; LIM, Dong Chul; KANG, Seung Wan; KIM, Hyung Jin; WO2010/93191; (2010); A2;,
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7135-31-1,2-Chloro-1H-indole,as a common compound, the synthetic route is as follows.

7135-31-1, General procedure: Intermediate 1-1 (5.0 g, 0.018 mol), 4-bromo-N,N-dip-tolylaniline (12.5 g, 0.036 mol), Pd(dba)2 (0.8 g, 0.0009 mol), sodium-tert-butoxide (3.5 g, 0.052 mol) in TOL 200 ml was reacted with stirring for 4 hours at 95 C. Reaction after H20:MC column purification after separation of to the compounds (n-HEXANE: MC) 11.2 g (75% yield) of compound 1 are obtained. 2-chloro-1H-indole (3.0 g, 0.020 mol) bromobenzene (3.1 g, 0.020 mol) for inserting and removing manufacturing e.g. in the embodiment 1-(2) the same method used in the synthesis of 3.3 g (73% yield) is obtained. (m/z=227)

The synthetic route of 7135-31-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; P&H tech; Hyeon, Seo Young; Jong, Song Ok; Oh, Hyeon Jin; (92 pag.)KR2015/131700; (2015); A;,
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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.245-08-9,5H-Pyrido[3,2-b]indole,as a common compound, the synthetic route is as follows.

Sub 1-3(4) round bottom flask (3.36g, 20mmol), Sub 1-2 (1) (4g, 20mmol), Pd2(dba) 3 (0.9g, 1mmol), PPh3 (0.5g, 2mmol) , the reaction proceeds at 100 C afterloading the NaOt-Bu (5.8g, 60mmol), toluene (210 mL). After completion of reaction,the organic layer was dried over MgSO4, and extracted with water and ether andrecrystallized silicagel column and the resulting organics concentrated to give 4.9g andthen the Sub 1 (B) -1. (Yield: 74%)

245-08-9, 245-08-9 5H-Pyrido[3,2-b]indole 6451402, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; DUK SAN NEOLUX CO., LTD.; PARK, JEONG KEUN; KIM, SEUL GI; PARK, HYOUNG KEUN; CHO, HYE MIN; PARK, JONG GWANG; KIM, SEOK HYEON; MOON, SOUNG YOON; LEE, TAE WON; (60 pag.)KR2015/121394; (2015); A;,
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

39974-94-2, 5-Methoxy-1-methyl-1H-indole-3-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Methoxy-1-methyl-1H-indole-3-carbaldehyde [76 g, Reference Example 2(a)] and hydroxylamine hydrochloride (55.9 g) were stirred together in dimethylformamide (900 mL) under reflux for 1 hour. The mixture was allowed to cool, then poured into water and then extracted with ethyl acetate. The combined extracts were washed with water then evaporated to give the title compound (53 g) as a pale brown solid, m.p. 100-104 C. 1H NMR [(CD3)2SO]: delta 8.17 (1H, s); 7.54 (1H, d, J=9.0 Hz); 7.09 (1H, d, J=2.4 Hz); 6.97 (1H, dd, J=9.0 and 2.4 Hz); 3.82 and 3.84 (6H, s)., 39974-94-2

39974-94-2 5-Methoxy-1-methyl-1H-indole-3-carbaldehyde 925973, aindole-building-block compound, is more and more widely used in various fields.

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Patent; Cox, Paul J.; Majid, Tahir N.; Lai, Justine Y.Q.; Morley, Andrew D.; Amendola, Shelley; Deprets, Stephanie D.; Edlin, Christopher; US2004/9983; (2004); A1;,
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

487-89-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.487-89-8,Indole-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

General procedure: To a dry dichloromethane solution (10 mL) of the appropriate 1H-indole-3-carbaldehydes(2 mmol), anhydrous potassium carbonate (6 mmol) and benzenesulfonyl chlorides (4 mmol) indry dichloromethane (20 mL) were added, and the mixture was stirred for 12 h at 40 C. After thecompletion of the reaction, excess solvent was removed under reduced pressure to obtain a yellowcrude solid of 3a-3b which was directly used in the next step without purification.

487-89-8 Indole-3-carboxaldehyde 10256, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Article; Song, Ming-Xia; Li, Song-Hui; Peng, Jiao-Yang; Guo, Ting-Ting; Xu, Wen-Hui; Xiong, Shao-Feng; Deng, Xian-Qing; Molecules; vol. 22; 6; (2017);,
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

247564-66-5, 4,6-Difluoroindole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of the above compound (3.0 g) and copper powder (2.9 g) in quinoline (30 ml) was stirred at 200 C. for 5 hours under argon atmosphere. After being cooled to room temperature, the insoluble materials were filtered off and washed with ethyl acetate (100 ml). The filtrate was washed with a 6 N aqueous hydrochloric acid solution twice and brine. The each aqueous layer was extracted with ethyl acetate, and the combined organic layer was dried over magnesium sulfate and treated with activated carbon. The insoluble materials were filtered off, and the filtrate was evaporated under reduced pressure. The residual oil was purified by silica gel column chromatography (hexane:ethyl acetate=10:1-6:1) to give 4,6-difluoroindole (2.60 g) as pale yellow oil. ESI-Mass m/Z 152 (M-H).

247564-66-5, 247564-66-5 4,6-Difluoroindole-2-carboxylic acid 3451441, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Tanabe Seiyaku Co., Ltd.; US2008/27122; (2008); A1;,
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

1074-86-8, 1H-Indole-4-carbaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

K2CO3 (19.2 g, 138.93 mmol) and 2-fluorobenzonitrile (9.18 g, 75.87 mmol) were added to a solution of 24 (10 g, 68.97 mmol) in 100 mL DMF. The mixture was stirred and refluxed for 1 h. After cooling to rt, the mixture was added to 100 mL water and extracted with ethyl acetate (100 mL * 3). After that the organic phase was collected and washed with NaCl saturated solution (150 mL * 5) and then dried over MgSO4. After filtration, the solvent was removed under reduced pressure. The residue was recrystallized by ethyl acetate to obtain white solid. Yield: 89.1percent. MP: 240-243 ¡ãC. 1H NMR (400 MHz, CDCl3) delta: 10.32 (s, 1H), 7.91 (d, 1H), 7.81 (t, 1H), 7.76 (d, 1H), 7.61-7.56 (m, 5H), 7.42 (t, 1H). MS (ESI): [M + H]+ calcd 247.1; found 247.2.

1074-86-8, As the paragraph descriping shows that 1074-86-8 is playing an increasingly important role.

Reference£º
Article; Zhu, Weibo; Bao, Xiaolu; Ren, He; Da, Yajing; Wu, Dan; Li, Fuming; Yan, Yijia; Wang, Li; Chen, Zhilong; European Journal of Medicinal Chemistry; vol. 115; (2016); p. 161 – 178;,
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

399-76-8, 5-Fluoroindole-2-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Fluorondole-2-carboxylic acid (5.00g, 27.91mmol) was added to ethanol (50mL) at 0 ¡ãC. SOCl2 (9.84g, 82.71mmol) was added to the mixture and the reaction mixture was warmed to reflux and stirred for 5 hours. TLC showed the reaction was complete, the reaction mixture was concentrated, and saturated aqueous NaHCO3 solution (15mL) was added thereto. The resulting mixture was extracted with DCM (100mL * 2) and the organic phase was dried over anhydrous sodium sulfate and concentrated to deliver the title compound (light yellow solid, 5.50g, yield 85.60percent). 1H-NMR (400 MHz, CDCl3) delta 9.00 (br. s., 1 H), 7.31 – 7.39 (m, 2 H), 7.19 (d, J=1.2Hz, 1 H), 7.10 (td, J=9.0, 2.4 Hz, 1 H), 4.43 (q, J=7.1 Hz, 2 H), 1.43 (t, J=7.1 Hz, 3 H)., 399-76-8

399-76-8 5-Fluoroindole-2-carboxylic acid 1820, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; GUANGDONG ZHONGSHENG PHARMACEUTICAL CO., LTD; DING, Charles Z.; CHEN, Shuhui; ZHAO, Baoping; LIU, Xile; XIAO, Linxia; DING, Chao; WANG, Fei; LI, Jian; (153 pag.)EP3290419; (2018); A1;,
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

271-34-1, 5-Azaindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-azaindole (5.00 g) and Et3N (12 mL) was added (Boc)20 ( 14 mL) dropwise at 0C. The mixture was stirred for 6 h, then diluted with water and extracted with EtOAc. The organic layer was dried over Na2S04 for 1 h and filtered. The filtrate was concentrated in vacuo and the residue was chromatographed with a silica gel column (eluting agent: 3: 1 (v/v) PE/EA) to give the title compound as transparent liquid (9.00 g, 97.00 %). The compound was characterized by the following spectroscopic data: ? NMR (400 MHz, CDC13) ?: 1.65 (s, 9H), 6.62 (d, J = 3.6 Hz, 1H), 7.25 (d, J = 5.3 Hz, 1 H), 7.50 (d, J = 3.5 Hz, 1H), 8.42 (d, J= 5.3 Hz, 1 H), 9.43 (s, lH) ppm., 271-34-1

The synthetic route of 271-34-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu; WO2013/71697; (2013); A1;,
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