相似化合物
477600-70-7 1354486-07-9 1228879-37-5欧盟法规
REACH注册ECHA物质C&L通报上下游产品
1-benzyl-4-methyl-piperidin-3-one methylamine methylamine acetate (1-benzyl-4-methyl-piperidin-3-yl)-methyl-amineTofacitinib citrate ((3R,4R)-4-methylpiperidin-3-yl)-N-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amine dihydr°Chloride tas°Citinib N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-(7-p-toluenesulfonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine 合成工艺路线路线简述
- 合成目标产物 (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine Dihydrochloride 主要起始原料 (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine
- (文献来源)合成步骤主要原料 (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine
专利信息
专利号:US-11827598-B1
优先权日:2022-07-15
标 题:Preparation method of tofacitinib citrate
发明人:HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present disclosure provides a preparation method of tofacitinib citrate, which comprises the following steps: passing an intermediate TOF-2 into hydrogen at a normal pressure in the presence of a catalyst to obtain an intermediate TOF-3; in the presence of a solvent and a base, under a reduced pressure of −490 mmHg to −760 mmHg, and at a temperature of 10° C. to 25° C., reacting TOF-3 with ethyl cyanoacetate to generate an intermediate TOF-4; heating and dissolving TOF-4 and citric acid in a solvent, and performing separation by cooling to obtain tofacitinib citrate. The present disclosure obtains tofacitinib citrate with high yield, high purity and low impurities by changing a gas flow rate and a reaction temperature and pressure of a hydrogenation reaction. Therefore, the preparation method is suitable for industrial production.
专利号:CN-113930404-A
优先权日:2021-10-13
标 题 :A kind of method for enzymatic synthesis of chiral tofacitinib citrate intermediate
专利号:CN-113930404-B
优先权日:2021-10-13
标题 :A method for enzymatic synthesis of chiral tofacitinib citrate intermediate
专利号:CN-108997199-B
优先权日:2018-08-13
标题:Synthesis method of tofacitinib intermediate (3R,4R) -1-benzyl-N, 4-dimethylpiperidine-3-amine