专利号:US-2012136015-A1 优先权日:2009-04-13 标题:Process for preparation of endothelial receptor antagonist (bosentan) 发明人:JOSHI SHREERANG; KHAN RASHID; BENDRE DEVEN; SALUNKHE DADASAHEB; GUDEKAR SANKET 权利人:JOSHI SHREERANG; KHAN RASHID; BENDRE DEVEN; SALUNKHE DADASAHEB; GUDEKAR SANKET; SANDOZ AG 摘要:The present invention relates to processes for the preparation of an endothelial receptor antagonist. The present invention particularly relates to synthesis of 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzene sulfonamide (bosentan).
专利号:US-2010256371-A1 优先权日:2009-04-02 标题:Processes for the preparation of bosentan and its intermediates thereof 发明人:YADAV ROOP SINGH; KHAN MUBEEN AHMED; LAD SACHIN MAHADEO; TRIVEDI NIKHIL RASIKLAL; ARJUNAN SANKAR; PITALE GAJENDRA LAXMAN 权利人:GLENMARK 摘要:The present invention relates to processes for the preparation of bosentan and compounds that can be used as structurally novel intermediates for the synthesis thereof, and a pharmaceutical composition of the same.
专利号:US-6004965-A 优先权日:1994-12-20 标题 :Sulfonamides 发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI 权利人:HOFFMANN LA ROCHE 摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
专利号:EP-2072503-B1 优先权日:2007-12-18 标题:Process for the preparation of bosentan 发明人:TADDEI MAURIZIO; NALDINI DILETTA; ALLEGRINI PIETRO; RAZZETTI GABRIELE; MANTEGAZZA SIMONE 权利人:DIPHARMA FRANCIS SRL 摘要:A process for the preparation of 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-[2,2']bipyrimidinyl-4-yl]-benzenesulfonamide, bosentan, comprising the reaction of a compound of formula ( II ) or a salt thereof, nwherein Z is an optionally protected hydroxy group, nwith a compound of formula ( III ), nin the presence of a base; and, if necessary, the removal of the hydroxy-protecting group, and/or, if desired, the conversion of a compound of formula (I) to a salt thereof, or vice versa ; and novel intermediates useful for its synthesis.
专利号:CN-117364108-A 优先权日:2023-10-19 标 题 :A simple multi-component preparation and synthesis method of N-sulfonylamidine compounds