CAS: 540737-29-9; 3-((3R,4R)-4-Methyl-3-(Methyl(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Amino)Piperidin-1-yl)-3-Oxopropanenitrile 2-Hydroxypropane-1,2,3-Tricarboxylate

上下游产品

(3R,4R)-methyl-(4-methyl-piperidin-3-yl)-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amine succinimidyl cyanoacetate citric acid tert-butyl (3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidine-1-carboxylate

4-氯-7H-吡咯并[2,3-D]嘧啶-7-羧酸叔丁酯置于氢气,Potassium Carbonate,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 甲醇,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 17.0H,反应生成 枸橼酸托法替尼
参考文献:一种枸橼酸托法替尼的制备方法
标题:一种枸橼酸托法替尼的制备方法
摘要:本发明涉及一种枸橼酸托法替尼的制备方法,具体涉及以4‑氯‑7‑吡咯并[2,3‑d]嘧啶,(Boc)2O,(3R,4R)‑(1‑苄基‑4‑甲基哌啶‑3‑基)甲胺‑l‑二对甲苯甲酰酒石酸盐,Pd/c,氰基乙酸和枸橼酸为原料,经氨基保护反应,氨基化反应,脱苄基反应,缩合反应,脱保护反应和成盐反应六步高产率合成枸橼酸托法替尼.本合成路线提供了一种枸橼酸托法替尼的制备方法是一种高收率,低成本,易操作,适宜工业化的制备方法.

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:CN-109503462-A
优先权日:2019-01-21
标 题:A new method for the synthesis of tofacitinib intermediate (3R,4R)-N,4-dimethyl-1-benzyl-3-piperidinamine and its oxalate hydrate

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:US-2024279179-A1
优先权日:2020-12-22
标题 :Synthesis and use of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivative