作者:Simon Woodward、Miriam Ackermann、Saurabh K. Ahirwar、Laurence Burroughs、Mary Robert Garrett、John Ritchie、Jonathan Shine、Björk Tyril、Kevin Simpson、Peter Woodward
DOI:10.1002/chem.201701170
日期:2017.6.7
described. The diverse cores (E)‐1,2‐Ar1CH2(HOCH2)C=C(CH2OH)I (Ar1=Ph, 4‐MePh, 4‐MeOPh, 4‐FPh) and (E)‐1,2‐I(HOCH2)C=C(CH2OH)I, accessed from ultra‐low cost HOCH2C≡CCH2OH at multi‐gram scales, allow the synthesis of diol libraries (E)‐1,2‐Ar1CH2(HOCH2)C=C(CH2OH)CH2Ar2 (Ar2=Ph, 4‐MePh, 4‐iPrPh, 4‐MeOPh, 4‐FPh, 4‐BrPh, 4‐biphenyl, 4‐styryl; 14 examples) by efficient Negishi coupling. Copper‐catalysed aerobic
描述了一种简单的区域特异性途径,该途径可替代地存在问题的取代的四碳烯。多种核(E)-1,2-Ar 1 CH 2(HOCH 2)C = C(CH 2 OH)I(Ar 1 = Ph,4-MePh,4-MeOPh,4-FPh)和(E) -1,2-I(HOCH 2)C = C(CH 2 OH)I,从超低成本HOCH访问2 C≡CCH 2 OH在多克规模,允许二醇库的合成(ë)-1- ,2-Ar 1 CH 2(HOCH 2)C = C(CH 2 OH)CH 2 Ar 2(Ar 2= Ph,4-MePh,4- i PrPh,4-MeOPh,4-FPh,4-BrPh,4-联苯,4-苯乙烯基; 14个示例)通过有效的Negishi耦合。铜催化的好氧氧化可干净地提供二醛(E)-1,2-Ar 1 CH 2(CHO)C = C(CHO)CH 2 Ar 2,在许多情况下,这些反应会经历氯化钛(IV)引起的双重Br