CAS: 51-73-0; 1,4-Di(Pyrrolidin-1-yl)But-2-Yne

📜四氢吡咯,1,4-二氯-2-丁炔 反应生成 1,1-(2-丁炔亚基)二吡咯烷二盐酸盐
参考文献:Hypotensive Agents. I. Acetylenic Diamines
标题:Hypotensive Agents. I. Acetylenic Diamines
摘要:
DOI:10.1021/ja01550A049

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:US-3896170-A
优先权日:1969-02-26
标题 :Intermediates for the preparation of 1,3-dihydro-2h-1, -benzodiazepin-2-ones
发明人：MCCAULLY RONALD J
权利人:AMERICAN HOME PROD
摘要:Two routes for the preparation of 2-(2-acylamido-2-amino)acetamidophenyl aryl ketones, used as intermediates in the synthesis of psycholeptic 1,3-dihydro-2H-1,4-benzodiazepin-2-ones are described. The first of these routes involves the formation of a 2-(2,2-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 corresponding 2-(2-acylamido-2halo)acetamidophenyl aryl ketone, and conversion to the 2-(2acylamido-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 2aminophenyl 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 vic glycol cleaving agent.

专利号:US-3883591-A
优先权日:1969-02-26
标 题:Intermediates for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones
发明人：MCCAULLY RONALD J
权利人:AMERICAN HOME PROD
摘要:Two routes for the preparation of 2-(2-acylamido-2-amino)acetamidophenyl aryl ketones, used as intermediates in the synthesis of psycholeptic 1,3-dihydro-2H-1,4-benzodiazepin-2-ones are described. The first of these routes involves the formation of a 2-(2,2-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, coversion 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 corresponding 2-(2-acylamido-2halo)acetamidophenyl aryl ketone, and conversion to the 2-(2acylamido-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 2aminophenyl 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 vic glycol cleaving agent.

专利号:US-3899527-A
优先权日:1969-02-26
标题:Intermediates for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones
发明人：MCCAULLY RONALD J
权利人:AMERICAN HOME PROD
摘要:Two routes for the preparation of 2-(2-acylamido-2-amino)acetamidophenyl aryl ketones, used as intermediates in the synthesis of psycholeptic 1,3-dihydro-2H-1,4-benzodiazepin-2-ones are described. The first of these routes involves the formation of a 2-(2,2-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 corresponding 2-(2-acylamido-2halo)acetamidophenyl aryl ketone, and conversion to the 2-(2acylamido-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 2aminophenyl 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 vic glycol cleaving agent.