公开(公告)号：WO2009137322A2

公开(公告)日：2009-11-12

申请号：PCT/US2009042243

申请日：2009-04-30

Applicant: UNIV PENNSYLVANIA ,  PERCEC VIRGIL ,  ROSEN BRAD MATTHEW ,  WILSON DANIELA A ,  WILSON CHRISTOPHER J

Inventor： PERCEC VIRGIL ,  ROSEN BRAD MATTHEW ,  WILSON DANIELA A ,  WILSON CHRISTOPHER J

IPC: C07C63/333 ,  C07F5/04

CPC classification number: C07F5/022 ,  C07C41/30 ,  C07C67/343 ,  C07C69/76 ,  C07C69/734 ,  C07C69/94 ,  C07C43/2055 ,  C07C43/205

Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aiyl; R3 -R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising: - contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs; - contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.

Abstract translation: 本发明涉及合成下式化合物的方法：其中：R 1和R 2各自独立地为C 1 -C 12烷基，CO 2 R 3，OR 4，R 5（OR 6）或C 6 -C 18芳基; R 3 -R 6各自独立地为C 1 -C 12烷基或C 6 -C 12芳基; 且n和m各自独立地为O或1-5的整数; 所述方法包括：在含镍催化剂存在下使式HO-R7-H的化合物与BH 3和下式化合物接触以产生第一产物，其中R 7是C 2 -C 12烃基，X 是卤素，OM或OT; - 将第一产物原位与下式化合物接触：在含镍催化剂存在下制备其中Z为卤素的式I化合物。

公开(公告)号：WO2009137322A3

公开(公告)日：2009-11-12

申请号：PCT/US2009/042243

申请日：2009-04-30

Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA ,  PERCEC, Virgil ,  ROSEN, Brad, Matthew ,  WILSON, Daniela, A. ,  WILSON, Christopher, J.

Inventor： PERCEC, Virgil ,  ROSEN, Brad, Matthew ,  WILSON, Daniela, A. ,  WILSON, Christopher, J.

IPC: A01N31/04 ,  A61K31/07 ,  A61K31/69

Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R 1 and R 2 are each, independently, C 1 -C 12 alkyl, CO 2 R 3 , OR 4 , R 5 (OR 6 ), or C 6 -C 18 aiyl; R 3 -R 6 are each, independently, C 1 -C 12 alkyl or C 6 -C 12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising: — contacting a compound of the formula H0-R 7 -0H with BH 3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R 7 is a C 2 -C 12 hydrocarbon group and X is a halogen, OMs or OTs; — contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.