Introduction of a new synthetic route about 10406-25-4

Statistics shows that 4-(Aminomethyl)benzonitrile is playing an increasingly important role. we look forward to future research findings about 10406-25-4.

Reference of 10406-25-4, These common heterocyclic compound, 10406-25-4, name is 4-(Aminomethyl)benzonitrile, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

General procedure: A sealed tube is charged with 7-chloro-5-(1 -methyl- 7 – -indol-6-yl)-quinoxaline (60.00 mg; 0.20 mmol; 1.0 eqr.) (Intermediate 4), 1-pyridin-3-yl-ethylamine (0.05 ml0.41 mmol; 2.0 eqf.), NaOtBu (58.77 mg; 0.61 mmol; 3.00 eqf.) and toluene (2.0 ml_). RM is purged with argon and then BINAP (25.39 mg; 0.04 mmol; 0.20 eqf.) and Pd2(dba)3 (18.67 mg; 0.02 mmol; 0.10 eq.) are added. RM is sealed and heated at 1 10C for 16 h. After this time, the mixture is filtered through a Celite pad and the filtrate is diluted with EtOAc and extracted with water. Combined organic phases are washed with brine, dried over Na2S04. Solvent is evaporated and the residue is purified by FCC (hexane/EtOAc; gradient). [8-(1 -Methyl- 7H-indol-6-yl)-quinoxalin-6-yl]-(1 – pyridin-3-yl-ethyl)-amine is obtained as a yellow powder (60.00 mg; yield 79%; 97% by HPLC).

Statistics shows that 4-(Aminomethyl)benzonitrile is playing an increasingly important role. we look forward to future research findings about 10406-25-4.

Reference:
Patent; SELVITA S.A.; FABRITIUS, Charles-Henry Robert Yves; NOWAK, Mateusz Oktawian; WIKLIK, Katarzyna Anna; SABINIARZ, Aleksandra Barbara; BIE?, Marcin Dominik; BUDA, Anna Ma?gorzata; GUZIK, Pawel Szczepan; JAKUBIEC, Krzysztof Roman; MACIUSZEK, Monika; KWIECI?SKA, Katarzyna; TOMCZYK, Mateusz Micha?; GA??ZOWSKI, Micha? Miko?aj; GONDELA, Andrzej; DUDEK, ?ukasz Piotr; (681 pag.)WO2016/180536; (2016); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts