2-氯吡嗪置于一水合肼体系中,化学反应 2.0H,以67%的收率获得产物吡嗪-2-肼 参考文献:Exploring The Unexplored Practical And Alternative Synthesis Of 3-(Trifluoromethyl)-Triazolopiperazine The Key Intermediate For Sitagliptin 标题:Exploring The Unexplored Practical And Alternative Synthesis Of 3-(Trifluoromethyl)-Triazolopiperazine The Key Intermediate For Sitagliptin 摘要:为了合成西格列汀的关键中间体3-(三氟甲基)-三唑并呱和3-(三氟甲基)-三唑吡啶,采用了工业上可行的转化方法进行实用合成.这种方法的另一个优点是通过消除常用的三氟乙酸酐和聚磷酸,提供了一种新型的环保合成三唑并呱和三唑吡啶的方法. DOI:10.2174/1570178611310050008
专利信息
专利号:US-10787458-B2 优先权日:2014-09-25 标 题:Chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-A]pyrazines 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:Disclosed is a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I): n nor a solvate thereof. The novel chiral synthesis avoids the use of protection/deprotection steps.
专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:US-2025034146-A1 优先权日:2023-07-13 标题:Electro-photochemical synthesis of 1,2,4-triazolo-[4,3-a]pyrazine 发明人:PIERCEY DAVIN GLENN; YOUNT JOSEPH ROBERT 权利人:PURDUE RESEARCH FOUNDATION 摘要:A method of preparing a 1,2,4-triazolo-[4,3-a]pyrazine backbone using an electro-photochemical process comprising coupling a compound comprising a 5-substituted tetrazole moiety to a compound comprising an optionally substituted pyrazine moiety electrochemically and subjecting the resulting compound to photochemical excitation with ultraviolet light.
专利号:US-11377359-B2 优先权日:2018-10-11 标题:Process for producing liquid polysilanes and isomer enriched higher silanes 发明人:NIKIFOROV GRIGORY; HUSSON GUILLAUME; ITOV GENNADIY; WANG YANG 权利人:AIR LIQUIDE; AIR LIQUIDE AMERICAN 摘要:Synthesis of silanes with more than three silicon atoms are disclosed (i.e., SinH(2n+2) with n=4-100). More particularly, the disclosed synthesis methods tune and optimize the isomer ratio by selection of process parameters such as temperature, residence time, and the relative amount of starting compounds, as well as selection of proper catalyst. The disclosed synthesis methods allow facile preparation of silanes containing more than three silicon atoms and particularly, the silanes containing preferably one major isomer. The pure isomers and isomer enriched mixtures are prepared by catalytic transformation of silane (SiH4), disilane (Si2H6), trisilane (Si3H8), and mixtures thereof.
专利号:US-2019218225-A1 优先权日:2014-09-25 标题:Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines
专利号:US-2017298070-A1 优先权日:2014-09-25 标题:Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines