Practical Selective Hydrogenation of α-Fluorinated Esters with Bifunctional Pincer-Type Ruthenium(II) Catalysts Leading to Fluorinated Alcohols or Fluoral Hemiacetals
作者:Takashi Otsuka、Akihiro Ishii、Pavel A. Dub、Takao Ikariya
DOI:10.1021/ja403852e
日期:2013.7.3
Selective hydrogenation of fluorinatedesters with pincer-type bifunctional catalysts RuHCl(CO)(dpa) 1a, trans-RuH2(CO)(dpa) 1b, and trans-RuCl2(CO)(dpa) 1c under mild conditions proceeds rapidly to give the corresponding fluorinatedalcohols or hemiacetals in good to excellent yields. Under the optimized conditions, the hydrogenation of chiral (R)-2-fluoropropionate proceeds smoothly to give the corresponding
METHOD FOR PRODUCING 4,4,7-TRIFLUORO-1,2,3,4-TETRAHYDRO-5H-1-BENZAZEPINE COMPOUND AND INTERMEDIATE USED IN THE METHOD
申请人:ASTELLAS PHARMA INC.
公开号:US20150141641A1
公开(公告)日:2015-05-21
The present invention provides a method for producing a 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound which has an superior agonistic activity to an arginine vasopressin V2 receptor and is useful as an active ingredient for a pharmaceutical composition for preventing and/or treating urinary frequency, urinary incontinence, enuresis, central diabetes insipidus, nocturia, nocturnal enuresis, or the like; and useful intermediates for use in the methods. The production method of the present invention is suitable for the industrial production of a medicament, because of a smaller number of steps, a higher yield, and a lower cost, as compared with the methods in the related art.