CHEMICAL SUBSTANCES WHICH INHIBIT THE ENZYMATIC ACTIVITY OF HUMAN KALLIKREIN-RELATED PEPTIDASE 6 (KLK6)
The invention relates to compounds which are suitable for the treatment of a disease associated with kallikrein-like peptidase 6 overexpression and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds or pharmaceutical compositions.
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Paragraph 0361; 0362
(2018/04/19)
Asymmetric borane reduction of ketones catalyzed by N-hydroxyalkyl-l-menthopyrazoles
The equimolar mixture of N-(hydroxyalkyl)pyrazoles and borane formed boric ester complex, in which the remaining borane was stabilized by the adjacent nitrogen of thr pyrazole ring. The borane complex derived from the chiral pyrazoles such as 3-phenyl-l-menthopyrazole reduced p-methylacetophenone (21) enantioselectively. When (2'S)-2-(2'-phenyl-2'-hydroxyethyl)-3-phenyl-l-menthopyrazole ((2'S)-10b) was used, 21 was reduced into (S)-p-methylphenyl-1-ethanol (22) in moderate chemical and optical yields. Due to the inconvenience of the preparation and the lower optical yield, the use of N-(α-hydroxyalkyl)pyrazoles was unpromising for the enantioselective reduction of ketones by borane.
Kashima,Tsukamoto,Higashide,Nakazono
p. 983 - 990
(2007/10/03)
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