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1. 发明申请

US20100125142A1 PROCESS FOR PREPARING AN OPTICALLY ACTIVE PROTON PUMP INHIBITOR 失效
标题翻译：制备光学活性原子泵抑制剂的方法
公开(公告)号：US20100125142A1
公开(公告)日：2010-05-20
申请号：US12451871
申请日：2008-05-30
申请人： Shankar Reddy Budidet , Brajesh Kumar Sinha , Somappa Somannavar Yallappa , Senthil Kumar Natarajan , Ramesh Dandala , Sivakumaran Meenakshisunderam
发明人： Shankar Reddy Budidet , Brajesh Kumar Sinha , Somappa Somannavar Yallappa , Senthil Kumar Natarajan , Ramesh Dandala , Sivakumaran Meenakshisunderam
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： An improved process for the preparation of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole of Formula I, (I) with high enantiomeric excess from racemic mixture.
摘要翻译：一种制备式（I）的（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑的方法，来自外消旋混合物的高对映体过量。

2. 发明申请

US20090281326A1 Process For the Preparation of Angiotensin II Antagonist 失效
标题翻译：血管紧张素II拮抗剂的制备方法
公开(公告)号：US20090281326A1
公开(公告)日：2009-11-12
申请号：US12309016
申请日：2007-06-29
申请人： Sankar Reddy Budidet , Senthil Kumar Natarajan , Venkata Kishore Gowrabathina , Ramesh Dandala , Sivakumaran Meenakshisunderam
发明人： Sankar Reddy Budidet , Senthil Kumar Natarajan , Venkata Kishore Gowrabathina , Ramesh Dandala , Sivakumaran Meenakshisunderam
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetra-zol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2′-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2′-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2′-(1-triphenylmethyl-tetra-=zol-5-yl)[1,1′biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2′-(1-H-tetrazol-5-yl)[1,1′biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by
摘要翻译：本发明提供了制备N-（1-氧代戊基）-N - [[2' - （1H-四唑-5-基）[1,1'-联苯] -4-基]甲基 ] -L-缬氨酸（缬沙坦），其包含用草酸或其水合物在溶剂中处理N - [[2' - （1-三苯基甲基 - 四唑-5-基）联苯-4-基]甲基] -L-缬氨酸甲酯（X），产生N - [[2' - （1-三 - 辛基甲基 - 四唑-5-基）联苯-4-基]甲基] -L-缬氨酸甲酯草酸酯（Xa）并用碱在溶剂中处理化合物（Xa）然后在碱存在下与戊酰氯在溶剂中反应，生成N - [[2' - （1-三苯基甲基 - 四 - 唑-5-基）[1,1'-联苯] -4-基]甲基] -N-缬氨酰-L-缬氨酸甲酯（XI），用无水酸性条件脱保护化合物（Ⅺ），得到N-（1-氧代戊基）-N - [[2' - （1-H- 吡啶-5-基）[1,1'-联苯] -4-基]甲基-L-缬氨酸甲酯（V），然后在溶剂中用碱处理以产生缬沙坦。

3. 发明授权

US07880015B2 Process for the preparation of angiotensin II antagonist 失效
标题翻译：制备血管紧张素II拮抗剂的方法
公开(公告)号：US07880015B2
公开(公告)日：2011-02-01
申请号：US12309016
申请日：2007-06-29
申请人： Sankar Reddy Budidet , Senthil Kumar Natarajan , Venkata Kishore Gowrabathina , Ramesh Dandala , Sivakumaran Meenakshisunderam
发明人： Sankar Reddy Budidet , Senthil Kumar Natarajan , Venkata Kishore Gowrabathina , Ramesh Dandala , Sivakumaran Meenakshisunderam
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetra-zol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2′-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2′-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2′-(1-triphenylmethyl-tetra-zol-5-yl)[1,1′biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2′-(1-H-tetrazol-5-yl)[1,1′biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by treating with base in a solvent to produce Valsartan.
摘要翻译：本发明提供了制备N-（1-氧代戊基）-N - [[2' - （1H-四唑-5-基）[1,1'-联苯] -4-基]甲基 ] -L-缬氨酸（缬沙坦），其包含用草酸或其水合物在溶剂中处理N - [[2' - （1-三苯基甲基 - 四唑-5-基）联苯-4-基]甲基] -L-缬氨酸甲酯（X），产生N - [[2' - （1-三 - 辛基甲基 - 四唑-5-基）联苯-4-基]甲基] -L-缬氨酸甲酯草酸酯（Xa）并用碱在溶剂中处理化合物（Xa）然后在碱存在下与戊酰氯在溶剂中反应，生成N - [[2' - （1-三苯基甲基 - 四唑-5-基）[1,1'-联苯] -4-基]甲基] N-缬氨酰-L-缬氨酸甲酯（XI），用无水酸性条件脱保护化合物（Ⅺ），得到N-（1-氧代戊基）-N - [[2' - （1-H-四唑-5 - 基）[1,1'-联苯] -4-基]甲基-L-缬氨酸甲酯（V），然后用溶剂中的碱处理，得到缬沙坦。

4. 发明授权

US08492551B2 Process for preparing an optically active proton pump inhibitor 失效
标题翻译：制备光学活性质子泵抑制剂的方法
公开(公告)号：US08492551B2
公开(公告)日：2013-07-23
申请号：US12451871
申请日：2008-05-30
申请人： Shankar Reddy Budidet , Brajesh Kumar Sinha , Somappa Somannavar Yallappa , Senthil Kumar Natarajan , Ramesh Dandala , Sivakumaran Meenakshisunderam
发明人： Shankar Reddy Budidet , Brajesh Kumar Sinha , Somappa Somannavar Yallappa , Senthil Kumar Natarajan , Ramesh Dandala , Sivakumaran Meenakshisunderam
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： An improved process for the preparation of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole of Formula I, (I) with high enantiomeric excess from racemic mixture.
摘要翻译：一种制备式（I）的（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑的方法，来自外消旋混合物的高对映体过量。

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