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    • 3. 发明申请
    • PROCESS FOR THE HYDROGENATION OF ESTERS OF ALPHA-SUBSTITUTED CARBOXYLIC ACIDS
    • 羟基取代的羧酸的加氢过程
    • WO2005023737A1
    • 2005-03-17
    • PCT/GB2004/003884
    • 2004-09-10
    • AVECIA LIMITEDMOODY, David, JohnHÄRRÖD, MagnusFIELDHOUSE, Robin
    • MOODY, David, JohnHÄRRÖD, MagnusFIELDHOUSE, Robin
    • C07C29/149
    • C07C29/149C07C67/31Y02P20/544C07C69/675C07C31/22C07C31/205
    • There is provided a process for the hydrogenation of esters of alpha-substituted carboxylic acids which comprises reacting an ester of an alpha-substituted carboxylic acid with hydrogen in the presence of a catalyst under substantially homogeneous supercritical conditions. Preferably, the ester of an alpha-substituted carboxylic acids is an ester of formula (1): wherein: R 1 and R 2 are each independently an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; and Y is a heteroatom or an optionally substituted heteroatom group. More preferably, the ester of an alpha-substituted is carboxylic acids is an ester of formula (2): wherein: R 3 is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; R 4 and R 5 are each independently hydrogen, an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; Y is a heteroatom or an optionally substituted heteroatom group; Q is a functional group; and n 1. Most preferably, the ester of an alpha-substituted carboxylic acids is an ester of formula (3): wherein: R 3 and R 6 are each independently an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; R 4 and R 5 are each independently hydrogen, an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; Y is a heteroatom or an optionally substituted heteroatom group; and n 1.
    • 提供了α-取代羧酸酯的氢化方法,其包括在催化剂存在下,在基本上均匀的超临界条件下使α-取代的羧酸的酯与氢反应。 优选地,α-取代的羧酸的酯是式(1)的酯:其中:R 1和R 2各自独立地为任选取代的烃基或任选取代的杂环基; 并且Y是杂原子或任选取代的杂原子基团。 更优选地,α-取代的酯是羧酸是式(2)的酯:其中:R 3是任选取代的烃基或任选取代的杂环基; R 4和R 5各自独立地为氢,任选取代的烃基或任选取代的杂环基; Y是杂原子或任选取代的杂原子基团; Q是功能组; 最优选地,α-取代的羧酸的酯是式(3)的酯:其中:R 3和R 6各自独立地是任选取代的烃基或任选取代的杂环基 ; R 4和R 5各自独立地为氢,任选取代的烃基或任选取代的杂环基; Y是杂原子或任选取代的杂原子基团; 和n 1。
    • 6. 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。
    • 9. 发明申请
    • PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ATORVASTATIN
    • 方法和中间体化合物在制备统计学,特别是ATORVASTATIN
    • WO2005012246A1
    • 2005-02-10
    • PCT/GB2004/003206
    • 2004-07-23
    • AVECIA LIMITEDMOODY, David, JohnWIFFEN, Jonathan, William
    • MOODY, David, JohnWIFFEN, Jonathan, William
    • C07D207/34
    • C07D405/06C07D207/34C07D309/10C07D309/30Y02P20/55
    • There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R 1 represents a hydrogen or a hydrocarbyl group, R 2 represents a hydrogen or substituent group, R 3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P 1 represents hydrogen or a protecting group, and W represents =0 or -OP 2 , in which P 2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents -OP 2 , deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents =O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof.
    • 提供了制备式(7)化合物或其盐的方法:其中R 1表示氢或烃基,R 2表示氢或取代基,R 3表示 氢或烃基,X表示氢或取代基,其包含a)氰化式(1)化合物:其中Y表示卤素基团,优选Cl或Br; P 1表示氢或保护基,W表示= 0或-OP 2,其中P 2表示氢或保护基,得到式(2)的化合物:b)将 式(2)化合物,得到式(3)化合物:将式(3)化合物与式(4)化合物偶合:得到式(5)化合物:当W表示-OP 2 然后氧化式(5)化合物,得到式(6)化合物:和e)当W表示= O时使式(5)的化合物或式(6)的化合物进行环 - 打开和除去任何剩余的保护基团,得到式(7)的化合物或其盐。