Abstract: The asymmetrical hydrogenation of 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolinium salts to yield (S) or (R)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinolinium salts can be effected with superior optical yield by the use of an iridium or rhodium complex catalyst comprising a chiral dipohsphine ligand of the general formula (I) or (II), (S)-1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-hexahydroisoquinoline and salts thereof are intermediate products in the manufacture of dextromethorphan, a known antitussive agent.

Abstract: The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) wherein Ra is hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II wherein R21 is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3 is bromo, chloro or iodo, and R1 is as above, with a vinyl borane compound in the presence of a Pd complex and a base, and optionally, further reacting a product of formula I wherein R2 is hydrogen with a compound of the formula IV wherein Rb is a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.

Abstract: Amino-amide ruthenium complexes of the general formula RuH(L′{—H})(Y) and RuX(L′{—H})(Y) wherein X signifies chlorine, bromine or iodine, Y signifies a neutral ligand, L′ signifies a monosulphonylated diamine of the general formula R1SO2—HN—CH2—(CH2)n—CH2—NHR4  II′ R1 signifies optionally mono- or multiply fluorinated alkyl, alkenyl, alkynyl, cycloalkyl, optionally mono- or multiply-substituted aryl, heteroaryl or camphor-10-yl, R4 signifies hydrogen or alkyl, and n signifies 0, 1, 2 or 3. is described.

Abstract: A process for the manufacture of trans-(R,R)-actinol by diasteroselective transfer hydrogenation of levodione comprises hydrogenating (R)-levodione in the presence of a hydrogen donor, which simultaneously can be used as the solvent, and an amino-amide-ruthenium complex, especially of the formula RuH(L{—H})(Y), wherein Y signifies a neutral ligand and L signifies an optionally optically active monosulphonylated diamine ligand, as defined in more detail in the description. Moreover, the invention is concerned with some of the amino-amide-ruthenium complexes and with the corresponding precursors to these complexes, which have halogen in place of H. The product of the process in accordance with the invention, trans-(R,R)-actinol, is known as an important building block for the synthesis of carotenoids, e.g. zeaxanthin. By the process trans-(R,R)-actinol is made available in particularly high enantiomeric and diasteromeric purity.