CAS: 96314-26-0; (2S,4S)-4-Phenylpyrrolidine-2-Carboxylic Acid

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90657-53-7 336818-78-1 269078-71-9

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CAS号3973-63-5 5-苯基哌啶-2-酮 | CAS号64-17-5 乙醇 | CAS号7732-18-5 水

📜Phenylmagnesium Bromide置于lithium,溶剂黄146体系中,用 四氢呋喃,二氯甲烷,三氟乙酸 作为反应溶剂,化学反应 38.17H,反应生成 反-4-苯基-L-脯氨酸
参考文献:Angiotensin-Converting Enzyme Inhibitors. Mercaptan,Carboxyalkyl Dipeptide,And Phosphinic Acid Inhibitors Incorporating 4-Substituted Prolines
标题:Angiotensin-Converting Enzyme Inhibitors. Mercaptan,Carboxyalkyl Dipeptide,And Phosphinic Acid Inhibitors Incorporating 4-Substituted Prolines
摘要:Analogues Of Captopril,Enalaprilat,And The Phosphinic Acid [hydroxy(4-Phenylbutyl)Phosphinyl]Acetyl]-L-Proline Incorporating 4-Substituted Proline Derivatives Have Been Synthesized And Evaluated As Inhibitors Of Angiotensin-Converting Enzyme (Ace) In Vitro And In Vivo. The 4-Substituted Prolines,Incorporating Alkyl,Aryl,Alkoxy,Aryloxy,Alkylthio,And Arylthio Substituents Were Prepared From Derivatives Of 4-Hydroxy-And 4-Ketoproline. In General,Analogues Of All Three Classes Of Inhibitors With Hydrophobic Substituents On Proline Were More Potent In Vitro Than The Corresponding Unsubstituted Proline Compounds. 4-Substituted Analogues Of Captopril Showed Greater Potency And Duration Of Action Than The Parent Compound As Inhibitors Of The Angiotensin I Induced Pressor Response In Normotensive Rats. The S-Benzoyl Derivative Of Cis-4-(Phenylthio)Captopril,Zofenopril,Was Found To Be One Of The Most Potent Compounds Of This Class And Is Now Being Evaluated Clinically As An Antihypertensive Agent. In The Phosphinic Acid Series,The 4-Ethylenethioketal And Trans-4-Cyclohexyl Derivatives Were Found To Be The Most Potent Compounds In Vitro And In Vivo. A Prodrug Of The Latter Compound,Fosinopril,Is Also Being Evaluated In Clinical Trials.
DOI:10.1021/jm00401A014

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:WO-2025128985-A1
优先权日:2023-12-14
标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.

专利号:US-11440881-B2
优先权日:2019-05-09
标题 :Thiosemicarbazates and uses thereof
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

专利号:US-2022372022-A1
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics