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    • 1. 发明申请
    • PROCESS FOR THE PREPARATION OF UNSATURATED ESTERS
    • 制备不饱和酯的方法
    • WO2004052823A1
    • 2004-06-24
    • PCT/GB2003/005332
    • 2003-12-08
    • AVECIA LIMITEDMOODY, David, JohnBAILEY, MarkBARRON, Sarah, Anne
    • MOODY, David, JohnBAILEY, MarkBARRON, Sarah, Anne
    • C07C67/00
    • C07C67/313C07C67/343Y02P20/55C07C69/66
    • A process for the preparation of an unsaturated ester of Formula (1); wherein: R 1 and R 2 are each independently hydroxy protecting groups; R 3 is optionally substituted C,_ 18 alkyl; R 4 is an organic group; and R 5 is H, an organic group or R 4 and R 5 together with the C atom to which they are attached form a ring which is a component of an organic group; which comprises reacting a compound of Formula (2); wherein R 1 , R 2 and R 3 are as defined above; with an oxidising agent in the presence of a compound of formula R 4 -CHR 5 -Y wherein R 4 and R 5 are as defined above and Y represents a group forming a Wittig reagent; a P, As or Sb-containing Horner-Wadsworth Emmons reagent; a P(III), As (III) or Sb(III) precursor of a Horner-Wadsworth Emmons reagent; a Warren reagent; or a ylid precursor; and optionally a base.
    • 制备式(1)的不饱和酯的方法; 其中:R 1和R 2各自独立地为羟基保护基; R 3是任选取代的C 1-8-18烷基; R 4是有机基团; R 5为H,有机基团或R 4和R 5与它们所连接的C原子一起形成作为有机基团的组分的环; 其包括使式(2)的化合物与 其中R 1,R 2和R 3如上所定义; 在式R 4 -CHR 5 -Y的化合物存在下与氧化剂反应,其中R 4和R 5如上所定义,Y代表形成Wittig试剂的基团; 一种含P,As或Sb的Horner-Wadsworth Emmons试剂; Horner-Wadsworth Emmons试剂的P(III),As(III)或Sb(III)前体; 沃伦试剂; 或前列腺素; 和任选的碱。
    • 2. 发明申请
    • COMPOUNDS AND PROCESSES
    • 化合物和方法
    • WO2004054986A2
    • 2004-07-01
    • PCT/GB2003/005359
    • 2003-12-09
    • AVECIA LIMITEDNEWTON, LeeBAILEY, Mark
    • NEWTON, LeeBAILEY, Mark
    • C07D239/00
    • C07D239/22C07C69/716C07D239/42C07D403/04
    • A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R 1 -CO-CH 2 -E with a compound of formula R 2 -CHX 1 X 2 in the presence of a compound of formula R 3 R 4 N-C(=NH)NH 2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (1). R 1 is H or an alkyl group; R 2 is H, an alkyl or aryl group; R 3 and R 4 are each independently H, alkyl or aryl, or R 3 and R 4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X 1 and X 2 are each independently leaving groups, or X 1 and X 2 together represent =O.
    • 提供了制备式(1)化合物和其中有用的中间体的方法。 该方法包括使式R 1 -CO-CH 2 -E的化合物与式R 2 -CHX 1 X 2的化合物在式R 3 R 2的化合物存在下反应, 4> NC(= NH)NH 2和催化剂,从而形成二氢嘧啶; 并氧化二氢嘧啶以形成式(1)的化合物。 R 1是H或烷基; R 2是H,烷基或芳基; R 3和R 4各自独立地为H,烷基或芳基,或R 3和R 4连接形成与它们所连接的氮一起形成5至7元杂环 环; E是H,未取代的烷基,芳基或吸电子基团; X 1和X 2各自独立地为离去基团,或X 1和X 2一起表示= O。