2-(4-甲基苯基)-1,3,4-恶二唑置于n-溴代丁二酰亚胺(Nbs),Sodium T-Butanolate,过氧化苯甲酰体系中,用 氯仿,N,N-二甲基甲酰胺 用作溶剂,化学反应 32.0H,反应生成对氰基溴化苄 参考文献:A Base-Induced Ring-Opening Process Of 2-Substituted-1,3,4-Oxadiazoles For The Generation Of Nitriles At Room Temperature 标题:A Base-Induced Ring-Opening Process Of 2-Substituted-1,3,4-Oxadiazoles For The Generation Of Nitriles At Room Temperature 摘要:A Novel Base-Catalysed 1,3,4-Oxadiazole Fragmentation For The Synthesis Of Nitriles At Room Temperature Has Been Developed. This Reaction Is Performed Under Transition-Metal-Free Conditions,And Provides A New Ring Cleavage Reaction Of 1,3,4-Oxadiazoles In Organic Synthesis. Doi:10.3184/174751914X14007780679741
专利号:US-9556140-B2 优先权日:2013-01-26 标 题 :Approach for synthesis of catechins 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH 权利人:SPHAERA PHARMA PRIVATE LTD 摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
专利号:US-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
专利号:US-9428482-B2 优先权日:2011-01-27 标 题 :Process for synthesis of polyphenols 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE; SPHAERA PHARMA PTE LTD 摘要:The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
专利号:WO-2010146391-A1 优先权日:2009-06-15 标题:Regioselective synthesis of letrozole 发明人:GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 权利人:GENERICS UK LTD; MYLAN INDIA PRIVATE LTD; GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 摘要:The present invention relates to an improved process for the preparation of letrozole (I) and its pharmaceutically acceptable salts, to compositions comprising letrozole or a pharmaceutically acceptable salt thereof, and to uses of such compositions. In particular it relates to a process and to novel intermediates for preparing letrozole and its salts substantially free from regioisomeric impurities.
专利号:US-7705159-B2 优先权日:2005-07-06 标题:Process for the preparation of letrozole 发明人:MACDONALD PETER LINDSAY; BIGATTI ETTORE; ROSSETTO PIERLUIGI; HAREL ZVI 权利人:SICOR INC 摘要:The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.