Day: March 16, 2022

162100-95-0, 6-Fluoro-5-methyl-1H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Diethylaluminium chloride 1M in hexane (15 mL, 15.1 mmol) was added dropwise at 000 to a solution of 6-fluoro-5-methyl-1 H-indole [CAS 162100-95-0] (1 .5 g, 10.6mmol) in CH2CI2 (30 mL). After 30 mm at 0C, 2-(4-fluoro-2-methoxyphenyl)acetyl chloride Ia? (3.05 g, 15.1 mmol, synthesis: see Example 1) in CH2CI2 (20 mL) was added slowly at 0C. The reaction was stirred at 0C for 3 h and then at room temperature for 1 h. Ice-water was added. The precipitate was filtered off, washed with water and dried under vacuum to afford 2-(4-fluoro-2-methoxyphenyl)-1 -(6-fluoro-5-methyl-1 H-indol-3-yl)ethanone 3a (2.27 g).

162100-95-0, 162100-95-0 6-Fluoro-5-methyl-1H-indole 2774611, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; JANSSEN PHARMACEUTICALS, INC.; KATHOLIEKE UNIVERSITEIT LEUVEN; BARDIOT, Dorothee Alice Marie-Eve; BONFANTI, Jean-Francois; COESEMANS, Erwin; KESTELEYN, Bart Rudolf Romanie; MARCHAND, Arnaud Didier M; RABOISSON, Pierre Jean-Marie Bernard; (96 pag.)WO2017/167952; (2017); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.39689-58-2,2-(1H-Indol-6-yl)acetic acid,as a common compound, the synthetic route is as follows.

39689-58-2, General procedure: to a solution of the substituted acid in DMF (0.25 mmol/mL) were added DMAP (2 to 4 equiv), EDCI.HCI (1 to 1.5 equiv) and the substituted amine (1 equiv). The reaction mixture was stirred at rt. After completion of the reaction (monitored by TLC), sat. NH4CI or HCI 0.5N was added and the solution was extracted with EtOAc. The organic layer was washed with sat. NH4CI, dried over Mg504, filtered and evaporated to dryness underreduced pressure (Figure 3AA).

As the paragraph descriping shows that 39689-58-2 is playing an increasingly important role.

Reference：
Patent; GENFIT; DELHOMEL, Jean-Francois; PERSPICACE, Enrico; MAJD, Zouher; PARROCHE, Peggy; WALCZAK, Robert; (284 pag.)WO2018/138362; (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

31241-19-7, 5-Methoxy-2,3,3-trimethyl-3H-indole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,31241-19-7

5-methoxy-2,3,3-trimethyl-3H-indole (2g, 10.6mmol) with1,4-butyl sultone (4.3 g, 31.7 mmol) was dissolved in 40 mL of toluene.The temperature was raised to 120 C and refluxed for 50 h.After the reaction, the mixture was filtered to give an off-white solid.Purified by column chromatography to give a pale yellow solid2-1 1.9g.

The synthetic route of 31241-19-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Shenyang Pharmaceutical University; Wang Dun; Wang Yongjun; Yang Xiaoguang; Lv Qingzhi; (25 pag.)CN108752319; (2018); 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

938465-52-2, 1-Chloro-5H-pyrido[4,3-b]indole-4-carboxamide is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

938465-52-2, To a solution of (S)-2-(4-fluorophenyl)-2,8-diazaspiro[5.Sjundecan-1-one (120 mg, 0.45 mmol) in NMP (3 mL) was added 1-chloro-5H-pyrido[4,3-bjindole-4-carboxamide(Intermediate 1, 123 mg, 0.Smmol) and DIPEA (174 mg, 1.35 mmol), and the mixture was heated under microwave irradiation for 1.5 h at 150 C.The mixture was purified with prepHPLC to give (R)- 1 -(8-(4-fluorophenyl)-7-oxo-2, 8-diazaspiro[5 .51 undecan-2-yl)-5H-pyrido [4,3- bjindole-4-carboxamide. MS: 472.3 [M+Hjt 1H NMR (400 MHz, CD3OD) 3 8.45 (s, 1H), 8.03 (d, fr8.0 Hz, 1H), 7.81 (d, fr8.0 Hz, 1H), 7.62 (t, J=7.3 Hz, 1H), 7.55 – 7.49 (m, 1H), 7.11 – 7.06(m, 4H), 4.28 (d, J=12.5 Hz, 1H), 4.03 – 3.93 (m, 1H), 3.87 (d, fr12.5 Hz, 1H), 3.80 (d, fr4.8Hz, 1H), 3.63 – 3.53 (m, 2H), 2.43 (ddd, fr4.8, 7.7, 12.9 Hz, 1H), 2.25 – 2.07 (m, 3H), 2.07 -1.98 (m, 3H), 1.94 – 1.84 (m, 1H) ppm.

938465-52-2 1-Chloro-5H-pyrido[4,3-b]indole-4-carboxamide 59198457, aindole-building-block compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; LIU, Jian; KOZLOWSKI, Joseph; KIM, Ronald; GAO, Xiaolei; BOGA, Sobhana Babu; YU, Younong; WU, Hao; LIU, Shilan; YANG, Chundao; (102 pag.)WO2016/164284; (2016); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1008-07-7,7-Chloro-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

We heated a mixture of (1-6) (1 mmol) and l-methylimidazol-255(l,3H)- dione (which we synthesized according to the method used by Janin et al., Eur. J. Org. Chem. 2002:1763-1769, 2002) (250mg, 2.5 mmol) in piperidine (2 mL) at 1100C for four hours under an argon atmosphere. Then, we allowed the reaction mixture to cool in a refrigerator (~ 5C) with the addition of ether (2 mL). We filtered the precipitate and washed it with ether to give (1-7). 1H NMR (500 MHz, DMSO-d6): delta 12.15 (IH, br s), 10.26 (IH, br s), 8.23 (IH, s), 7.79 (IH, d, J = 8.0 Hz), 7.27 (IH, d, J = 8.0 Hz,), 7.13 (IH, t, J = 7.8 Hz), 6.82 (IH, s), 2.97 (3H, s).

1008-07-7, The synthetic route of 1008-07-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; PRESIDENT AND FELLOWS OF HARVARD COLLEGE; THE BRIGHAM AND WOMEN’S HOSPITAL, INC.; WO2007/75772; (2007); 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