4,4-Dimethyl-2-(4'-Methylbiphenyl-2-yl)Oxazoline置于盐酸,N-溴代丁二酰亚胺(Nbs),氯化亚砜,叠氮基三甲基硅烷,N,N-二异丙基乙胺,三苯基膦,Sodium Hydroxide,偶氮二甲酸二乙酯体系中,用 四氢呋喃,甲醇,四氯化碳,水 用作溶剂,化学反应生成N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑 参考文献:1,(3,)5-Substituted Imidazoles,Useful In The Treatment Of Hypertension And Methods For Their Preparation 标题:1,(3,)5-Substituted Imidazoles,Useful In The Treatment Of Hypertension And Methods For Their Preparation
专利号:EP-1546135-B1 优先权日:2002-07-16 标题:Novel synthesis of irbesartan 发明人:NISNEVICH GENNADY; RUKHMAN IGOR; PERTSIKOV BORIS; KAFTANOV JULIA; DOLITZKY BEN-ZION 权利人:TEVA PHARMA 摘要:Provided is a novel synthesis of irbesartan employing a phase transfer catalyst. Also provided is irbesartan having a fine particle size.
专利号:US-7312340-B2 优先权日:2003-02-05 标 题:Synthesis of 2-butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one 发明人:DOLITZKY BEN-ZION; KAFTANOV JULIA; PERTSIKOV BORIS; RUKHMAN IGOR; NISNEVICH GENNADY 权利人:TEVA PHARMA 摘要:Provided is a novel method of making 2-butyl-3-[[2′(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.
专利号:WO-2006038223-A1 优先权日:2004-10-06 标题:A process for preparation of 2-n-butyl -4-chloro - 1 - {[2`- (2-triphenylmethyl - 2h - tetrazole - 5- yl) - 1, 1’ - biphenyl-4-yl] methyl}-lh- imidazoie-5-methanol (intermediate of losartan) 发明人:CHAVA SATYANARYANA; VASIREDDY UMAMAHESWAR RAO; VELLANKI SIVA RAM PRASAD; BALUSU RAJABABU 权利人:MATRIX LAB LTD; CHAVA SATYANARYANA; VASIREDDY UMAMAHESWAR RAO; VELLANKI SIVA RAM PRASAD; BALUSU RAJABABU 摘要:The present invention relates to a process for preparation of N-substituted heterocyclic derivative,2-n-Butyl-4-chloro- 1 - { [2' -(2-triphenylmethyl-2H-tetrazole-5-yl)- 1,1' -biphenyl -4-yl] methyl} -lH-imidazole-5-methanol, an important intermediate in the synthesis of Losartan and its pharmaceutically acceptable salts using phase transfer catalyst and minimal number of solvents with improved yield.
专利号:EP-1831186-B1 优先权日:2004-11-30 标题:A process for the synthesis of valsartan 发明人:ZUPANCIC SILVO; PECAVAR ANICA; ZUPET ROK 权利人:KRKA D D NOVO MESTO 摘要:This invention relates to an improved process for preparing a valsartan, or a pharmaceutically acceptable salt thereof, or pharmaceutical preparation containing either entity wherein a compound of formula (II) nor a salt thereof, is reacted with valine or an ester or a salt thereof in a solvent selected from the group consisting of methylene chloride, chloroform, butyl chloride, isopropyl acetate and tert -butyl methyl ether to form a compound of formula (IV) nwhich is then acylated to form a compound of formula (VI) nwherein R is hydrogen, alkyl, alkenyl or benzyl; which is then deprotected to give valsartan, and may be converted to a pharmaceutically acceptable salt and/or a pharmaceutical formulation. The invention also covers intermediates of formula (IV) and (VI) wherein R=H.
专利号:US-2006128967-A1 优先权日:2003-02-05 标 题:Novel synthesis of 2-Butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one
专利号:US-7906501-B2 优先权日:2004-04-28 标题:Pyrrole derivatives with angiotensin II antagonist activity 发明人:MAKOVEC FRANCESCO; ARTUSI ROBERTO; GIORDANI ANTONIO; ZANZOLA SIMONA; ROVATI LUCIO CLAUDIO 权利人:ROTTAPHARM SPA 摘要:Compounds which may be represented by the general formula (I) shown below and in which: R 1 is a group independently selected from among: CHO, —COOH, —CH 2 OH R 2 is hydrogen or a linear or branched C 1 -C 6 alkyl group R 3 is hydrogen or a halogen group selected from among Cl and Br R 4 is a linear or branched C 3 -C 5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT 1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
参考标题:Improved Sommelet Reaction Catalysed By Lanthanum Triflate 作者:Wenhao Xu,Weike Su |发布日期:2014.12 摘要:An Improved Sommelet Reaction For The Synthesis Of Araldehydes From Benzyl Halides And Hexamethylenetetramine Was Achieved Employing Lanthanum Triflate (3 Mol%) As Catalyst In Water With Sodium Dodecyl Sulfate (Sds, 2 Wt%) As Solubiliser. Good To Excellent Yields Were Obtained In Most Of The 18 Examples.