CAS: 7729-30-8; (R)-Azetidine-2-Carboxylic Acid

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CAS号249734-37-0 BENZYL [1(1S),2... | CAS号1758-80-1 L-2,4-二氨基丁酸氢溴酸盐 | CAS号228857-58-7 (R)-N-B°C-氮杂环丁烷-2-羧酸

📜1-苄氧羰基-氮杂环丁烷-2-甲酸置于palladium On Activated Charcoal 氢气体系中,用 甲醇 作为反应溶剂,化学反应 72.0H,反应生成 D-吖啶-2-羧酸
参考文献:Identification And Initial Structure−activity Relationships Of (R)-5-(2-Azetidinylmethoxy)-2-Chloropyridine (Abt-594),A Potent,Orally Active,Non-Opiate Analgesic Agent Acting Via Neuronal Nicotinic Acetylcholine Receptors
标题:Identification And Initial Structure−activity Relationships Of (R)-5-(2-Azetidinylmethoxy)-2-Chloropyridine (Abt-594),A Potent,Orally Active,Non-Opiate Analgesic Agent Acting Via Neuronal Nicotinic Acetylcholine Receptors
摘要:New Members Of A Previously Reported Series Of 3-Pyridyl Ether Compounds Are Disclosed As Novel,Potent Analgesic Agents Acting Through Neuronal Nicotinic Acetylcholine Receptors. Both (R)-2-Chloro-5-(2-Azetidinylmethoxy)Pyridine (Abt-594,5) And Its S-Enantiomer (4) Show Potent Analgesic Activity In The Mouse Hot-Plate Assay Following Either Intraperitoneal (Ip) Or Oral (Po) Administration,As Well As Activity In The Mouse Abdominal Constriction (Writhing) Assay,A Model Of Persistent Pain. Compared To The S-Enantiomer And To The Prototypical Potent Nicotinic Analgesic Agent (+/-)-Epibatidine,5 Shows Diminished Activity In Models Of Peripheral Side Effects. Structure-Activity Studies Of Analogues Related To 4 And 5 Suggest That The N-Unsubstituted Azetidine Moiety And The 2-Chloro Substituent On The Pyridine Ring Are Important Contributors To Potent Analgesic Activity.
DOI:10.1021/jm9706224

专利信息

专利号:US-2023391818-A1
优先权日:2020-11-05
标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.

专利号:WO-2023214577-A1
优先权日:2022-05-02
标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.

专利号:US-7691843-B2
优先权日:2002-07-11
标 题 :N-hydroxyamide derivatives possessing antibacterial activity
发明人：RAJU BORE G; O'DOWD HARDWIN; GAO HONGWU; PATEL DINESH V; TRIAS JAOQUIM
权利人:PFIZER
摘要:Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.

专利号:CN-111334083-B
优先权日:2018-12-18
标 题:A Class of Reactive Fluorescent Dyes with High Brightness and High Stability and Their Synthesis and Application

专利号:CN-111334077-B
优先权日:2018-12-18
标题:A kind of high brightness, high stability fluorescent dye excited by 488nm and its synthesis method

专利号:CN-111333576-B
优先权日:2018-12-18
标题 :A class of highly stable wash-free Halo-tag probes and their synthesis and biological applications