CAS: 133909-99-6; Trityl Losartan

上下游产品

2-n-butyl-4-chloro-5-hydroxymethylimidazole tetrazoleN-(triphenylmethyl)-5-4'-(bromomethyl)biphenyl-2-yltetrazole trityl chloride 2-n-Butyl-4-chloro-1-[(2'-cyanobiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imidazolelorsartan 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole cozaar triphenylmethyl alcohol

咪唑醛置于sodium Tetrahydroborate,Potassium Carbonate体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 48.0H,反应生成三苯甲基洛沙坦
参考文献:非肽血管紧张素ii受体拮抗剂:发现了一系列n-(联苯基甲基)咪唑类有效的口服活性降压药.
标题:非肽血管紧张素ii受体拮抗剂:发现了一系列n-(联苯基甲基)咪唑类有效的口服活性降压药.
摘要:制备了一系列新的非肽血管紧张素ii(aii)受体拮抗剂.这些n-(联苯基-甲基)咪唑,例如2-丁基-1-[[(2'-羧基联苯-4-基)甲基]-4-氯-5-(羟甲基)咪唑,不同于先前报道的n-(苯甲酰氨基苄基)咪唑和相关化合物,因为它们在口服时产生有效的降压作用;较早的系列通常仅在静脉内给药时才有效.已经发现联苯的2'-位的酸性基团是必不可少的.仅邻位取代的酸具有对aii受体的高亲和力和非常好的口服降压效能.羧酸基团已被各种酸性等排体取代,并且发现四唑环是最有效的.四唑衍生物dup 753
Doi:10.1021/jm00112A031

专利信息

专利号:US-2008214637-A1
优先权日:2004-11-11
标题 :Process for the Synthesis of Tetrazoles
发明人：ANTONCIC LJUBOMIR; LUDESCHER JOHANNES
权利人:LEK PHARMACEUTICALS
摘要:A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.

专利号:WO-2004087691-A1
优先权日:2003-04-03
标题:A process for the synthesis of losartan potassium
发明人：KUMAR ASHOK; SINGH RAJESH KUMAR; PANDA NALINAKSHYA; UPARE ABHAY ATMARAM; NIMBALKAR MANMOHAN MADHAVRAO; SOUDAGAR SATISH RAJANIKANT
权利人:IPCA LAB LTD; KUMAR ASHOK; SINGH RAJESH KUMAR; PANDA NALINAKSHYA; UPARE ABHAY ATMARAM; NIMBALKAR MANMOHAN MADHAVRAO; SOUDAGAR SATISH RAJANIKANT
摘要:A process for the synthesis of Losartan Postassium by reacting Trityl Losartan in a primary alcohol with potassium tertiary alkoxide.

专利号:US-6916935-B2
优先权日:2003-05-06
标题 :Losartan potassium synthesis
发明人：KUMAR ASHOK; SINGH RAJESHKUMAR; PANDA NALINAKSHYA; UPARE ABHAY; NIMBALKAR MANMOHAN; SOUDAGAR SATISH
权利人:IPCA LAB
摘要:A process for the synthesis of Losartan Potassium by reacting Trityl Losartan in a primary alcohol with potassium tertiary alkoxide.

专利号:US-7345071-B2
优先权日:2003-05-07
标题 :Process for the synthesis of Losartan potassium
发明人：KUMAR ASHOK; SINGH RAJESH KUMAR KESHAVA PRA; PANDA NALINAKSHYA BALARAM; UPARE ABHAY ATMARAM; NIMBALKAR MANMOHAN MADHAVRAO; SOUDAGAR SATISH RAJANIKANT; SAXENA ASHVINI KUMAR NAND KISH
权利人:IPCA LAB LTD
摘要:Improved processes using primary, secondary and tertiary alcohols and with safer mode of introduction of the reagent and reaction conditions are described. Further, the process of manufacture of Losartan potassium by use of alkali metal salt such as Potassium carbonate is disclosed. A process for preparation of the polymorphic Form I of Losartan potassium is also disclosed herein.

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:US-5130439-A
优先权日:1991-11-18
标题:Tetrazolylphenylboronic acid intermediates for the synthesis of AII receptor antagonists
发明人：LO YOUNG S; ROSSANO LUCIUS T
权利人:LO YOUNG S; ROSSANO LUCIUS T
摘要:Novel tetrazolylphenylboronic acids, methods for their preparation, and their use in the syntheses of angiotensin II receptor antagonists are disclosed.