【结 构 式】 |
【分子编号】59821 【品名】ethyl (2S)-2-[(cyanomethyl)amino]propanoate 【CA登记号】 |
【 分 子 式 】C7H12N2O2 【 分 子 量 】156.18456 【元素组成】C 53.83% H 7.74% N 17.94% O 20.49% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(XVI)The chiral piperazine building block (XVIII) was prepared as follows. L-Alanine ethyl ester (XV) was condensed with formaldehyde and NaCN to give the amino nitrile (XVI). Catalytic hydrogenation of the cyano group of (XVI) with simultaneous intramolecular cyclization furnished the piperazinone (XVII). This was reduced to the target (S)-2-methylpiperazine (XVIII) by means of LiAlH4 (1).
【1】 Iwata, M.; Kimura, T.; Inoue, T.; Fujihara, Y.; Katsube, T. (Sankyo Co., Ltd.; Ube Industries, Ltd.); 4-Oxoquinoline-3-carboxylic acid derivs., their preparation and their use. AU 8938218; EP 0352123; EP 0610958; JP 1990124873; JP 1990231476; JP 1993255183; US 5002947; US 5073556; US 5348961 . |
Extended Information