发明名称 |
AN IMPROVED PROCESS FOR THE PREPARATION OF (3R,4R)-(1-BENZYL-4-METHYLPIPERIDIN-3-YL)-METHYLAMINE |
摘要 |
The present invention is related to an improved and efficient process for preparation of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine which comprises: (a) N-acylation of 3-Amino-4-methyl pyridine; (b) Quarternization of 3-Acetylamino-4- methyl pyridine using benzyl halide; (c) Partial reduction of quarternized 3-Acetylamino- 4-methyl pyridine by Sodium borohydride in Methanol or water; (d) Hydrolysis of partially reduced product to 1-Benzyl-4-methylpiperidin-3-one in presence of acid; (e) Reductive animation of 1-Benzyl-4-methylpiperidin-3-one using Methanolic methylamine in presence of Titanium(IV) isopropoxide in Methanol; (f) Resolution of 1-Benzyl-4- methylpiperidin-3-yl)-methylamine using Ditoluoyl (L) tartaric acid to get (3R,4R)-(1- benzyl-4-methylpiperidin-3-yl)-methylamine. The invention is also related to novel intermediates. |
申请公布号 |
WO2015087201(A1) |
申请公布日期 |
2015.06.18 |
申请号 |
WO2014IB66510 |
申请日期 |
2014.12.02 |
申请人 |
UNICHEM LABORATORIES LIMITED |
发明人 |
SATHE, DHANANJAY. G.;DAS, ARIJIT;PATIL, YOGESH SUBHASH;BONDE, NILESH L.;KEKAN, ANKUSH SAMPAT |
分类号 |
C07D211/56;C07D213/74 |
主分类号 |
C07D211/56 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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