CAS: 622-30-0; N-Benzylhydroxylamine

该化合物是一种有机化合物,其特征是存在一个苯基组和一个羟基胺功能组,似乎是白到白的晶状固体,可溶于水和酒精等极地溶剂,该化合物以其作为减少剂的作用而著称,经常用于有机合成,特别是用于制备氨和其他含氮化合物;Benzylhylxylamine也可以作为核分裂剂,因为存在氢氧基胺组,使其在各种化学反应中有用,包括形成氧化氮和氨,此外,该化合物在医药化学和合成药物中作为中间剂也有应用,但是,与许多有机化合物一样,该化合物应谨慎处理,因为如果浸入或吸入,可能会对健康造成危害,而且在使用该化合物时,应观察适当的安全措施.

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合成工艺路线路线简述

    苯甲醛肟置于盐酸,Sodium Cyanoborohydride体系中,用 甲醇,水 作为反应溶剂,化学反应生成 N-苄基羟胺
    参考文献:Sc(otf)3催化硝基酮与炔酮的[3 + 2]-环加成
    标题:Sc(otf)3催化硝基酮与炔酮的[3 + 2]-环加成
    摘要:一种有效的方法来获得官能化的(2,3-二氢异恶唑-4-基)酮,是通过使硝酮4与ynones 7或末端ynones 10以一锅法反应来开发的.反应经过正式的sc(otf)3催化的[3 + 2]-环加成过程,反应生成许多官能化的(2,3-Dihydroisoxazol-4-Yl)酮11Aa-11Aw,11Ba-11La和12Aa-12Ae产量中等至非常好.
    DOI:10.1039/d0Ob02158J

    海关参考信息

    专利信息


    专利号:EP-2666771-A1
    优先权日:2012-05-24
    标题 :Synthesis of Aminocyclopentanetriol Derivatives
    发明人:STERK DAMJAN; CASAR ZDENKO
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor. nThe present invention provides in particular a process for the preparation of a compound of formula Vn ncomprising: na) providing a compound of formula IVn n, and nb) reducing the compound of formula IV with activated zinc in the presence of copper to give the compound of formula V.

    专利号:US-9278972-B2
    优先权日:2011-12-23
    标题 :Synthesis of triazolopyrimidine compounds
    发明人:MARAS NENAD; GAZIC SMILOVIC IVANA; STERK DAMJAN
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.

    专利号:US-6133409-A
    优先权日:1996-12-19
    标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
    发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
    权利人:AVENTIS PHARM PROD INC
    摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

    专利号:US-6710208-B2
    优先权日:1996-12-19
    标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds
    发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
    权利人:AVENTIS PHARMA INC
    摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

    专利号:US-2004101523-A1
    优先权日:1989-07-27
    标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

    专利号:WO-9101724-A1
    优先权日:1989-07-27
    标题 :Renal-selective prodrugs for the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
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    合成参考文献


    摘要:Collier, S. J.; Singh, S. K., Science of Synthesis, (2010) 45, 83.
    摘要:Merino, P., Science of Synthesis Knowledge Updates, (2010) 4, 354.
    摘要:Merino, P., Science of Synthesis Knowledge Updates, (2010) 4, 345.
    摘要:Merino, P., Science of Synthesis Knowledge Updates, (2010) 4, 340.
    摘要:Johnson, J. B., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 811.
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