《Enantioselective Synthesis of a 2,3-Benzodiazepine Intermediate of BET Inhibitor BAY 1238097 via Catalytic Asymmetric Hydrogenation》 was written by Verzijl, Gerard K. M.; Hassfeld, Jorma; de Vries, Andre H. M.; Lefort, Laurent. Product Details of 126456-43-7 And the article was included in Organic Process Research & Development in 2020. The article conveys some information:
Herein, we report the first example of the asym. hydrogenation of a prochiral benzodiazepine substrate as key transformation in a pilot-scale synthesis of BET inhibitor BAY 1238097 (I). High-throughput screening in a parallel reactor enabled us to identify an efficient catalyst based on Ir and a chiral bisphosphine. An additive screening allowed significant reduction of catalyst loading. Ultimately, the hydrogenation was performed on a kilogram scale leading to the production of 27 kg of the desired product with an enantiomeric excess of 99% after crystallization In the experiment, the researchers used (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7Product Details of 126456-43-7)
(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Product Details of 126456-43-7
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts