A process is described for preparing a compound of Formula (1.3.0):
comprising: establishing a reaction mixture consisting of
in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; followed by heating said reaction mixture under a nitrogen atmosphere;
in a preferred embodiment the aprotic solvent is DMSO, the strong base in solid form is NaOH in powder or pellet form, and the phase transfer catalyst is tetra-n-butylammonium chloride (TBAC);
wherein the starting material of Formula (2.0.0) is prepared as follows:
are reacted together in a solvent consisting of a straight or
branched chain aliphatic alcohol; in the presence of a strong base consisting of NaOH or KOH; further in the presence of a transition metal catalyst comprising a palladium metal complex; and still further in the presence of an auxiliary ligand comprising a bidentate, chiral, axially dissymmetric aromatic compound of Formula (5.5.0) or (5.5.1):
本发明描述了一种制备式(1.3.0)化合物的工艺:
包括
在非沸腾溶剂中;在 NaOH 或 KOH 存在下;可选择在相转移催化剂,特别是季
铵盐或
鏻盐存在下; 然后在氮气环境下加热所述反应混合物;
在一个优选的实施方案中,
壬烷溶剂为
二甲基亚砜,固体形式的强碱为粉末状或颗粒状的 NaOH,相转移催化剂为四正丁基
氯化铵(
TBAC);
其中式(2.0.0)的起始原料按如下方法制备:
在由直链或支链
脂肪醇组成的溶剂中一起反应
在由直链或支链
脂肪醇组成的溶剂中;在由 NaOH 或 KOH 组成的强碱存在下;进一步在由
钯金属络合物组成的过渡
金属催化剂存在下;以及进一步在由式 (5.5.0) 或 (5.5.1) 的双齿、手性、轴向不对称芳香化合物组成的辅助
配体存在下: