The hydrogenation of 2-methylquinoline with Ir catalysts based on chiral phosphine-phosphites has been investigated. It has been observed that the reaction is very sensitive to the nature of the ligand. Optimization of the catalyst, allowed by the highly modular structure of these phosphine-phosphites, has improved the enantioselectivity of the reaction up to 73% ee. The influence of additives ...

Condensation and cyclization of 5-hydroxy- 1,2,4- thiadiazol-2-yl hydrazine 1 with pyruvic acid, phenacyl bromide, propargyl bromide and ally1 bromide afforded compounds 2,5,7 3, 4 ,6 and 8 respectively, Reaction of 1 with epichforohydrine afforded 4-hydroxy-N-[5-hydroxy- 1 ,3,4-thiadiazoly1] pyrazolidine 9