CAS: 477600-73-0; N-((3R,4R)-1-Benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine

相似化合物

1260590-51-9 477600-74-1 1655430-59-3

上下游产品

托法替布相关杂质22 (1-Benzyl-4-Methyl-Piperidin-3-yl)-Methyl-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-Amine 384337-90-0
N-(1-Benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7-Tosyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 1252883-87-6
托法替尼 Intb3 N-((3R,4R)-1-Benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7-Tosyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 923036-30-0

4-甲基-1-(苯基甲基)-3-哌啶酮置于二对甲苯酰基-L-酒石酸,Potassium Carbonate,Sodium Hydroxide体系中,用 甲醇,水,异丙醇,乙腈 作为反应溶剂,化学反应 13.0H,反应生成 (3R,4R)-(1-苄基-4-甲基-哌啶-3-基)-甲基-(7H-吡咯并[2,3-D]嘧啶-4-基)-胺
参考文献:一种枸橼酸托法替布中间体及枸橼酸托法替布的制备方法
标题:一种枸橼酸托法替布中间体及枸橼酸托法替布的制备方法
摘要:本发明公开了一种枸橼酸托法替布中间体及枸橼酸托法替布的制备方法.所述枸橼酸托法替布中间体的制备方法为:以3‑氨基‑4‑甲基‑吡啶,乙酰氯,氯化苄和硼氢化钠为原料,制备得到n‑(1‑苄基‑4‑甲基‑1,2,5,6‑四氢哌啶‑3‑基)乙酰胺;以n‑(1‑苄基‑4‑甲基‑1,2,5,6‑四氢哌啶‑3‑基)乙酰胺,盐酸,甲胺和硼氢化钠为原料,制备得到1‑苄基‑n,4‑二甲基哌啶‑3‑胺;1‑苄基‑n,4‑二甲基哌啶‑3‑胺经过拆分,游离,与盐酸成盐步骤后,即得.本发明提供了一种新的枸橼酸托法替布中间体的制备方法,且在枸橼酸托法替布制备过程中,降低了催化氢化催化剂用量,从而降低成本;采用异丙醇\水混合溶剂可以较好的控制n‑烷基化杂质的反应生成.

专利信息

专利号:US-8309716-B2
优先权日:2005-07-29
标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis
发明人：RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J
权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER
摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

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:US-9828380-B2
优先权日:2015-04-10
标题 :Efficient method for the preparation of tofacitinib citrate
发明人：BONANOMI JACOPO; DEFIORE STELLA; NOVO BARBARA
权利人:OLON SPA
摘要:Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises:n 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)

专利号:CN-105693728-A
优先权日:2014-11-29
标 题:Synthesis method of JAK inhibitor tofacitinib