专利号:US-8426612-B2 优先权日:2009-04-22 标 题:Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole 发明人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO 权利人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO; ITALIANA SINT SPA 摘要:The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
专利号:WO-2005103035-A1 优先权日:2004-04-23 标题:Modified fischer indole synthesis of eletriptan 发明人:ASHCROFT CHRISTOPHER PAUL 权利人:PFIZER LTD; ASHCROFT CHRISTOPHER PAUL; PFIZER 摘要:The present invention relates to a new process for the preparation of eletriptan (I), or its enantiomer comprising a modified Fischer indole synthesis, namely the reaction of a compound of formula (II), wherein R1 is a suitable hydrazine protecting group, with a compound of formula (III) wherein R2 is an aldehyde group (-CHO) or the functional equivalent thereof.
专利号:EP-2647639-A1 优先权日:2012-04-06 标题:ß-boration of alkene and alkyne intermediates 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-borated compounds can be used as intermediates in the synthesis of pharmaceutically active agents such as Sitagliptin.
专利号:EP-2647640-A1 优先权日:2012-04-06 标 题:ß-boration of alkene and alkyne intermediates 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-boated compounds can be used as intermediates in the synthesis of pharmaceutically active agents such as Sitagliptin.
专利号:US-9006231-B2 优先权日:2008-03-03 标 题:Cephalotaxus esters, methods of synthesis, and uses thereof 发明人:GIN DAVID Y; WILMOT JEREMY; DJABALLAH HAKIM 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
专利号:WO-2010121673-A1 优先权日:2009-04-22 标 题 :Synthesis of 3-{[(2r)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1h-indole