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公开(公告)号:US06573387B1
公开(公告)日:2003-06-03
申请号:US09381407
申请日:2000-01-31
申请人: K. Barry Sharpless , A. Erik Rubin
发明人: K. Barry Sharpless , A. Erik Rubin
IPC分类号: C07D20304
CPC分类号: C07D203/22 , C07C231/12 , C07C231/16 , C07C303/40 , C40B40/04 , C40B50/08 , C07C311/19
摘要: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.
摘要翻译: α,β-不饱和酰胺和酯转化为α,β-取代的氨基酰胺,酯和酸。 首先使用锇催化的氨基羟基化将α,β-不饱和酰胺或酯转化为α,β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯。 然后将α,β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯环化脱水以产生α,β-N-磺酰基或α,β-N-氨基甲酰基氮丙啶酰胺或酯。 然后将氮丙啶中间体环以区域选择性方式用各种亲核试剂进行亲核打开,得到$ g(α,β-取代的氨基酰胺或酯)。优选的亲核试剂包括硫,氧,碳和氮亲核试剂。
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公开(公告)号:US06573388B1
公开(公告)日:2003-06-03
申请号:US10069318
申请日:2002-02-18
申请人: Byung Moon Kim , Sung Jin Bae , Soon Mok So , Jae Sung Kang , Joong Hwan Lee
发明人: Byung Moon Kim , Sung Jin Bae , Soon Mok So , Jae Sung Kang , Joong Hwan Lee
IPC分类号: C07D20304
CPC分类号: C07D307/20 , C07C271/16 , C07D203/10 , C07D303/36 , C07F7/1804 , C07F7/1892 , Y02P20/55
摘要: This invention is related to new ethylaziridine derivatives of formula (I) and their preparation. The compounds are useful synthetic intermediates for the synthesis of HIV protease inhibitors and oligopeptide mimetics.
摘要翻译: 本发明涉及式(I)的新的乙基氮丙啶衍生物及其制备方法。 该化合物是用于合成HIV蛋白酶抑制剂和寡肽模拟物的合成中间体。
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公开(公告)号:US06566534B2
公开(公告)日:2003-05-20
申请号:US09984466
申请日:2001-10-30
申请人: Yoshihisa Oka , Kenichi Takematsu
发明人: Yoshihisa Oka , Kenichi Takematsu
IPC分类号: C07D20304
CPC分类号: C07D203/02
摘要: In order to carry out various vapor-phase reactions (e.g., the preparation of aziridine compounds by a vapor-phase intramolecular dehydration reaction) with industrial advantages, there is provided a process which can effectively prevent the adhesion of tarry matter to piping and the like. This process is applicable, for example, to the preparation of aziridine compounds by using a reactor for carrying out the vapor-phase intramolecular dehydration reaction of an alkanolamine, a collection column for collecting an aziridine compound present in the reaction gas, and a distillation column for distilling the collector liquid to obtain a purified aziridine compound, and is characterized in that at least the piping section extending from the outlet of the reactor to the inlet of the collection column is maintained at a temperature which is not lower than 200° C., or in that the reaction gas is brought into contact with a collector prior to its introduction into the collection column.
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