CAS: 63999-80-4; 2-Amino-3-(3-Cyanophenyl)Propanoic Acid

上下游产品

CAS号191872-32-9 N-B°C-DL-3-氰基苯丙氨酸

3-Cyano-Dl-Phenylalanine Methyl Ester Hydrochloride置于盐酸,溶剂黄146体系中,化学反应 2.0H,反应生成 3-氰基苯丙氨酸
参考文献:Synthesis And Structure−activity Relationships Of Potent Thrombin Inhibitors: Piperazides Of 3-Amidinophenylalanine
标题:Synthesis And Structure−activity Relationships Of Potent Thrombin Inhibitors: Piperazides Of 3-Amidinophenylalanine
摘要:Thrombin Is The Key Enzyme In The Blood Coagulation System,And Inhibitors Of Its Proteolytic Activity Are Of Therapeutic Interest Since They Are Potential Anticoagulants. The Most Potent Inhibitor Of The Benzamidine Type Is N-Alpha-[(2-Naphthylsulfonyl)Glycyl]-4-Amidinophenylalanylpiperidide (Napap). However,Napap And Other Benzamidine Derivatives Do Not Show Favorable Pharmacological Properties; Above All,They Have Very Low Systemic Bioavailability After Oral Administration. The Goal Of Designing New Compounds Was To Obtain Potent Inhibitors With Improved Pharmacokinetic Properties. Piperazide Derivatives Of 3-Amidinophenylalanine As The Key Building Block Were Synthesized. The Piperazine Moiety Opened The Possibility To Introduce Quite Different Substituents On The Second Nitrogen Using Common Synthetic Procedures. Some Of The Newly Synthesized Compounds Are Potent Inhibitors Of Thrombin And Offer An Approach To Study Structure-Function Relationships For Inhibition Of Thrombin And Related Enzymes And For The Improvement Of Their Pharmacokinetic Properties.
DOI:10.1021/jm960668H

专利信息

专利号:US-9938509-B2
优先权日:2010-12-08
标 题 :Biocatalysts and methods for the synthesis of armodafinil
发明人：ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN
权利人:CODEXIS INC
摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.

专利号:US-9663771-B2
优先权日:2013-01-18
标题 :Engineered biocatalysts useful for carbapenem synthesis
发明人：SUKUMARAN JOLY; SMITH DEREK; YANG HONG; YEO WAN LIN; MOORE JEFFREY C
权利人:CODEXIS INC
摘要:The present disclosure provides engineered pNB esterase polypeptides useful for the synthesis of the carbapenem antibiotic, imipenem. The disclosure also provides polynucleotides encoding the engineered pNB esterases, host cells capable of expressing the engineered pNB esterases, and methods of using the engineered pNB esterases in the production of imipenem.

专利号:US-12410410-B2
优先权日:2015-02-10
标题 :Ketoreductase polypeptides for the synthesis of chiral compounds
发明人：ALVIZO OSCAR; AGARD NICHOLAS J; XIE XINKAI; ENTWISTLE DAVID; KOSJEK BIRGIT
权利人:CODEXIS INC
摘要:The present disclosure provides engineered ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzymes, host cells capable of expressing the engineered ketoreductase enzymes, and methods of using the engineered ketoreductase enzymes to synthesize a variety of chiral compounds.

专利号:US-8932838-B2
优先权日:2010-06-17
标 题 :Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol
发明人：CABIROL FABIEN LOUIS; GOHEL ANUPAM; OH SEONG HO; SMITH DEREK J; WONG BRIAN; LALONDE JAMES J
权利人:CODEXIS INC
摘要:The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.

专利号:US-8932836-B2
优先权日:2010-08-16
标 题:Biocatalysts and methods for the synthesis of (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine
发明人：LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK
权利人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK; CODEXIS INC
摘要:The disclosure provides transaminase polypeptides capable of converting the substrate, 2-(3,4-dimethoxyphenethoxy)cyclohexanone to the trans diastereomer product (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine in at least a 2:1 diastereomeric ratio relative to the cis diastereomer (1R,2S)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine. The disclosure also provides polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides in processes for preparing (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine and its analogs, which can product compounds can be further used to prepare the aminocyclohexylether compound, (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol, which is an ion channel blocker.

专利号:US-9624478-B2
优先权日:2011-09-08
标题:Biocatalysts and methods for the synthesis of substituted lactams
发明人：CABIROL FABIEN LOUIS; CHEN HAIBIN; GOHEL ANUPAM; SALIM PAULINA ELENA; SMITH DEREK J; JANEY JACOB; KOSJEK BIRGIT; TANG WENG LIN; HSIEH HELEN; PHAM SON Q
权利人:CODEXIS INC
摘要:The present disclosure relates to transaminase polypeptides capable of aminating a dicarbonyl substrate, and polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides.