On September 28, 2006, Koppel, Gary; Miller, Marvin published a patent.SDS of cas: 53838-27-0 The title of the patent was Preparation of oxoazetidineacetic acid derivatives as human vasopressin V1a receptor antagonists for the treatment of premenstrual disorders. And the patent contained the following:
Oxoazetidineacetic acid derivatives I [R1 = H, alkyl; R2 = H, alkyl, alkoxy, alkylthio, NC, OHC, alkylcarbonyl, (un)substituted aminocarbonyl; R3 = (un)substituted amino, amido, or ureido; R4 = (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, alkylcarbonyl, aralkyl, etc.; R5 = R7, R7CO; R6 = HO, HS, HO2C, (un)substituted ester, amide, alc., or thiol derivatives; R7 = HO2C, (un)substituted carboxylic acid ester or amide, carboxyalkyl, alkoxycarbonylalkyl, (un)substituted aminocarbonylalkyl], particularly (oxazolidinyl)(oxo)azetidineacetic acid derivatives such as II, are prepared as antagonists of human vasopressin V1a receptors for use in the treatment and prevention of premenstrual disorders. The preparation of I uses stereoselective [2+2] cycloadditions of ketenes generated from oxazolidinyl-substituted acid chlorides and amino acid-derived imines as the key steps. Data on the binding of the title compounds to human vasopressin V1a receptors is given; for example, II binds human vasopressin V1a receptors with an IC50 value of 1.84 nM. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).SDS of cas: 53838-27-0
The Article related to oxoazetidineacetic acid nonracemic preparation vasopressin v1a receptor antagonist, premenstrual disorder treatment vasopressin v1a receptor antagonist oxoazetidineacetic acid, beta lactamyl alkanoic acid preparation treatment premenstrual disorder and other aspects.SDS of cas: 53838-27-0
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