Downstream synthetic route of 434958-85-7

434958-85-7 N-Boc-5-Hydroxyindole 22596220, aindole-building-block compound, is more and more widely used in various fields.

434958-85-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.434958-85-7,N-Boc-5-Hydroxyindole,as a common compound, the synthetic route is as follows.

Step 4: 1H-indole-1-carboxylic acid 5-[(dichlorophosphinyl)oxy]-1,1-dimethylethyl ester; To tert-butyl 5-hydroxy-1H-indole-1-carboxylate in Et2O (0.11 M) was added TEA (1.0 eq.), this solution was cooled to -78 C., then phosphorous oxychloride (1.0 eq) was added neat at that temperature and the resulting solution was left to warm to room temperature overnight. The white slurry was filtered under an inert atmosphere of N2 and all volatiles removed to yield the title compound as a colorless liquid that was used as is for the next step.31P NMR (300 MHz, CDCl3, 300K): delta4.23.

434958-85-7 N-Boc-5-Hydroxyindole 22596220, aindole-building-block compound, is more and more widely used in various fields.

Reference:
Patent; MacCoss, Malcolm; Olsen, David B.; Donghi, Monica; Gardelli, Cristina; Harper, Steven; Meppen, Malte; Narjes, Frank; Pacini, Barbara; US2010/234316; (2010); 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