CAS: 477600-70-7; (3R,4R)-1-Benzyl-N,4-Dimethylpiperidin-3-Amine

上下游产品

CAS号1092578-34-1 tert-butyl (3R,...

4-甲基-1-(苯基甲基)-3-哌啶酮置于盐酸,Bis(1,5-Cyclooctadiene)Diiridium(I) Dichloride,氢气,Sodium Hydroxide,(R)-Dime-Pipphos体系中,用 乙醚,乙醇,水,异丙醇,丙酮 作为反应溶剂,20.0 °C,5.0 Mpa 条件下,反应 24.0H,反应生成 顺式1-苄基-4-甲基-3-甲氨基-哌啶
参考文献:托法替尼关键中间体的不对称合成,通过动态动力学拆分-还原胺化方案进行
标题:托法替尼关键中间体的不对称合成,通过动态动力学拆分-还原胺化方案进行
摘要:我们报告了在动态动力学分辨率(dkr)条件下制备手性胺作为tofacitinib(一种由辉瑞公司开发的活性药物成分的关键中间体)的关键中间体的催化不对称还原胺化的第一个例子.这样的方案允许从相应的外消旋酮开始,从四种可能的手性胺的非对映异构体中优先形成单个产物.通过高通量筛选,外消旋研究和反应优化相结合,发现了能够进行此类盛宴的手性铱催化剂.
DOI:10.1021/acs.Oprd.8B00332

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-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