Tacurion

Astellas Pharma Gmbh

Kiichi Sato

Takahiro Akiba

Hiroyuki Koshio

Souichirou Kawazoe

Kazuyoshi Obitsu

Junji Itoh

Akio Miyafuji

Shun Hirasawa

Hiroshi Ikeda

Shuichi Nakagawa

Takashi Kikuchi

Shinya Yoshida

Toshitaka Yoshino

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.

Method for producing 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound and intermediate used in the method

Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production.

Method for producing sulfonyl amidine compound

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Tokyo, Japan

Kiichi Sato