CAS: 1022-13-5; (5-Chloro-2-(Methylamino)Phenyl)(Phenyl)Methanone

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CAS号719-59-5 2-氨基-5-氯二苯甲酮 | CAS号77-78-1 硫酸二甲酯 | CAS号28195-03-1 N-methyl-3-phen... | CAS号36271-03-1 N-(2-benzoyl-4-... | CAS号201230-82-2 carbon monoxide | CAS号74-88-4 碘甲烷 | CAS号78823-14-0 N-(N-phthaloyl-... | CAS号64-17-5 乙醇 | CAS号54888-03-8 2-acetamido-N-(... | CAS号57180-64-0 2-(methylamino-... | CAS号439-14-5 地西泮 | CAS号67057-48-1 2-(N-methyl)ami... | CAS号5621-63-6 (2-amino-3,5-di... | CAS号23751-99-7 (5-chloro-2-(di... | CAS号719-59-5 2-氨基-5-氯二苯甲酮 | CAS号34659-75-1 6-chloro-1-meth... | CAS号20927-53-1 6-chloro-1-meth... | CAS号5973-28-4 7-氯-1-甲基-3,4-二氢... | CAS号6021-21-2 2-(N-甲基氯乙酰氨)-5-氯二苯甲酮

去甲西泮置于盐酸,水,Sodium Methylate,Lithium Diisopropyl Amide体系中,用 四氢呋喃,甲醇,正己烷 用作溶剂,化学反应 18.5H,反应生成2-甲氨基-5-氯二苯甲酮
参考文献:
标题:
摘要:The Aldol Reaction Of The C(3) Carbanion Of 7-Chloro-1,3-Dihydro-1-Methyl-5-Phenyl-2H-1,4-Benzodiazepin-2-One (2) With A Series Of Aromatic And Aliphatic Aldehydes At-78 Degrees Afforded Threolerythro Diastereoisomers 3-16 Of 7-Chloro-1,3-Dihydro-3-(Hydroxymethyl)-1-Methyl-5-Phenyl-2H-1,4-Benzodiazepinones,Substituted At The C(3) Side Chain,In A Ratio From 55:45 To 94:6 (Scheme 1). Lewis Acids Exhibited Limited Effect On The Syn/ Anti Diastereoselectivity Of This Reaction,And Kinetic Control Of The Reaction Was Confirmed. H-1-NMR Data Suggested The Assignment Of The Threo Relative Configuration To The First-Eluted Diastereoisomers 3,5,7,And 9 On Reversed-Phase HPLC,And The Erythro Configuration To The Second-Eluted Counterparts 4,6,8,And 10,Respectively. The Structures And Relative Configurations Three And Erythro Of The Diastereoisomers 5 And 6,Respectively,Were Established By Single-Crystal X-Ray Analysis,Confirming The Assignment Based On The H-1-NMR Data. A Tentative Mechanistic Explanation Of The Diastereoselectivity Invokes The Enolate Anion Of 1,3-Dihydro-2H-1,4-Benzodiazepin-2-One As The Reactive Species (Scheme 2). Acid-Catalyzed Hydrolytic Ring Opening Of 3 Afforded Threo-Beta-Hydroxy-Phenylalanine 17,Whereas From 4,The N-(Benzyloxy)Carbonyl Derivative 18 Of Erythro-Beta-Hydroxy-Phenylalanine Was Obtained (Scheme 3); In Both Cases,Neither Elimination Of H2O From The C(3)-Choh Moiety Nor Epimerization At C(3) Were Observed. This Result Opens A New Pathway To Various Configurationally Uniform Alpha-Amino-Beta-Hydroxy Carboxylic Acids And Their Congeners Of Biological Importance.
Doi:10.1002/(Sici)1522-2675(20000315)83:3<603::Aid-Hlca603>3.0.Co;2-1

专利信息

专利号:US-3763171-A
优先权日:1969-02-26
标 题:Preparation of intermediates for the preparation of 1,3 - dihydro - 2h-1,4-benzodiazepin-1-ones
发明人：MC CAULLY R
权利人:AMERICAN HOME PROD
摘要:TWO ROUTES FOR THE PREPARATION OF 2-(2-ACYLAMINDO-2AMINO)-ACETAMIDOPHENYL ARYL KETONES, USED AS INTERMEDIATES IN THE SYNTHESIS OF PSYCHOLEPTIC 1,3-DIHYDRO-2H1,4-BENZODIAZEPIN-2-ONES ARE DESCRIBED. THE FIRST OF THESE ROUTES INVOLVES THE FORMATION OF A 2-N2,2-DIACYLOXY) ACETAMIDOPHENYL ARYL KETONE FROM GLYOXYLIC ACID AND AN ARYL PHENYL KETONE VIA EITHER A 2,2-DIACYLOXY ACETYL HALIDE OR A 2,2-DIACYLOXY ACETYL ANHYDRIDE, CONVERSION THEREOF TO THE CORRESPONDING 2-(2-ACYLAMIDO-2-HYDROXY)ACETAMIDOPHENYL ARYL KETONE DIRECTLY OR VIA THE 2-(2,2-DIHYDROXY) ACETAMIDOPHENYL ARYL KETONE, FORMATION OF THE CORRSPONDING 2-(2-ACYLAMIDO-2-HALO) ACETAMIDOPHENYL ARYL KETONE, AND CONVERSION TO THE 2-(2-ACYLAMIDO-2-AMINO) ACETAMIDOPHENYL ARYL KETONE. THE SECOND ROUTE FORMS THE 2-(2,2-DIHYDROXY) ACETAMIDOPHENYL ARYL KETONE BY REACTING A 2,3-DICARBOXYLICACYL TARTARIC ANHYDRIDE WITH A 2-AMINOPHENYL ARYL KETONE TO OBTAIN A 2-(3-CARBOXY-2,3ACYLOXY) PROPIONAMIDOPHENYL ARYL KETONE, SELECTIVELY HYDROLYZING THE SO-OBTAINED KETONE AND SELECTIVELY OXIDIZING THE PRODUCT WITH A VIX GLYCOL CLEAVING AGENT.

专利号:CN-117229206-A
优先权日:2023-09-18
标 题 :A preparation method for base-catalyzed synthesis of multi-substituted 2-quinolinone compounds