CAS: 149709-62-6; 4-(((2S,4R)-1-([1,1'-Biphenyl]-4-yl)-5-Ethoxy-4-Methyl-5-Oxopentan-2-yl)Amino)-4-Oxobutanoic Acid

上下游产品

CAS号149690-05-1 沙库巴曲钠 | CAS号128779-47-5 (R)-3-([1,1'-联苯... | CAS号76757-90-9 丁氧羰基-D-酪氨酸-甲氧基酯 | CAS号149818-98-4 N-叔丁基氧基羰基-氨基-4,...

Lcz700杂质置于水,Sodium Carbonate体系中,用 乙醇 用作溶剂,化学反应 6.0H,以80%的收率获得沙库巴曲
参考文献:一种抗心衰药物沙库巴曲的合成工艺
标题:一种抗心衰药物沙库巴曲的合成工艺
摘要:本发明公开了一种抗心衰药物沙库巴曲的合成工艺,所述合成工艺具体步骤为:(1)化合物v与乙醇,在浓硫酸存在的条件下,反应生成化合物vi;(2)化合物vi在碱存在下与丁二酰亚胺发生迈克尔加成反应,生成化合物vii;(3)化合物vii经水解生成化合物i;即所述沙库巴曲.本发明合成工艺中起始物料易得,且操作简单,整个合成过程污染小,易分离纯化,便于放大剂量实现工业化生产,且目标产物的收率更高,合成成本更低廉.

专利信息

专利号:WO-2017033128-A1
优先权日:2015-08-25
标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors
发明人：HOOK DAVID; KU JIE; ZHOU JIANGUANG
权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG
摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.

专利号:WO-2017051326-A1
优先权日:2015-09-23
标 题 :New processes and intermediates useful in synthesis of nep inhibitors
发明人：MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
权利人:NOVARTIS AG; MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors such as sacubitril, and prodrugs thereof.

专利号:US-10851059-B2
优先权日:2016-08-17
标题:Processes and intermediates for NEP inhibitor synthesis
发明人：KLEINBECK-RINIKER FLORIAN KARL; MAFLI IVES; MARTIN BENJAMIN; PENN GERHARD; SEDELMEIER GOTTFRIED; SEDELMEIER JOERG; VENTURONI FRANCESCO
权利人:NOVARTIS AG
摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.

专利号:US-10385004-B2
优先权日:2015-02-13
标 题:Process and intermediates for the preparation of NEP inhibitors
发明人：MARTIN BENJAMIN; MANDRELLI FRANCESCA; VENTURONI FRANCESCO
权利人:NOVARTIS AG
摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

专利号:US-12297462-B2
优先权日:2017-06-14
标 题:Engineered transaminase polypeptides for industrial biocatalysis
发明人：NOVICK SCOTT J; DELLAS NIKKI; ALVIZO OSCAR; Garcia Ravi David; CHING CHARLENE; ENTWISTLE DAVID
权利人:CODEXIS INC
摘要:The present invention provides engineered transaminase polypeptides useful for the synthesis of chiral amine compounds under industrially relevant conditions. The invention also provides polynucleotides encoding the engineered transaminase polypeptides, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases for the production of chiral amine compounds.

专利号:CN-108203396-A
优先权日:2016-12-19
标 题 :Synthesis of a Neprilysin Inhibitor