CAS: 158747-02-5; (R)-Frovatriptan

上下游产品

(R)-3-[benzyl(Methyl)Amino]-2,3,4,9-Tetrahydro-1H-Carbazole-6-Carboxamide 158747-18-3

📜(R)-3-[benzyl(Methyl)Amino]-2,3,4,9-Tetrahydro-1H-Carbazole-6-Carboxamide置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 用作溶剂,化学反应 1.0H,以71%的收率获得夫罗曲坦
参考文献:血清素受体激动剂 (R)-Frovatriptan 的化学酶促不对称合成
标题:血清素受体激动剂 (R)-Frovatriptan 的化学酶促不对称合成
摘要:已经开发了一种简单的化学酶促不对称途径来生产抗偏头痛药 (R)-Frovatriptan.脂肪酶和氧化还原酶已被确定为在安全和环境友好的条件下生产对映体纯的合成中间体的理想生物催化剂.(S)-3-Hydroxy-2,3,4,9-Tetrahydro-1H-Carbazole-6-Carbonitrile 是该药物合成的最佳结构单元,已通过 Candida Antarctica 脂肪酶 B 型催化酰化其相应的外消旋混合物或醇脱氢酶a介导相应酮的生物还原.手性中心的反转已被确定为关键步骤,优化过程以避免部分外消旋化.最后,
Doi:10.1002/ejoc.201300114

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-6787668-B2
优先权日:2000-04-13
标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors
发明人：PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH
权利人:PHARMACIA CORP
摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:WO-0134561-A1
优先权日:1999-11-06
标 题:Processes for the preparation of sumatriptan and related compounds
发明人：HOLMAN NICHOLAS JOHN; FRIEND CHRISTOPHER LYNDON
权利人:KNOLL AG; HOLMAN NICHOLAS JOHN; FRIEND CHRISTOPHER LYNDON
摘要:The present invention relates to a process for preparing phenylhydrazines of formula (I) in which R represents CH2SO2NHCH3, CH2CH2SO2Ph, CH2CH2SO2NHMe or a group of structure (A), (B), (C), in which a diazonium salt of formula (II) in which X represents an anion derived from hydrochloric acid, sulphuric acid, acetic acid, phosphoric acid, tetrafluoroboric acid or hydrobromic acid is reduced by a dithionite salt. The resulting phenylhydrazines can be converted to the corresponding indole derivatives by the Fischer indole synthesis.