Eisai Company, Limited

Other

Akio Kayano

Shigeto Negi

Manabu Sasho

Masahiko Tsujii

Hiroyuki Chiba

Taiju Nakamura

Shin Sakurai

Hiroyuki Ishizuka

Hiroyuki Saito

Hiroshi Kuroda

Naoyuki Shimomura

Katsuya Tagami

Hiroyuki Naka

Nobuaki Sato

Yasuyuki Suzuki

Kazuhide Ashizawa

Ken Furukawa

Kazuhiro Yoshizawa

Hirofumi Kuroda

Nobuo Niikawa

Ikuo Kushida

Masahiro Sakurai

Eiichi Yamamoto

Toyokazu Haga

Yuuki Komatsu

Takako Yoshiba

Manabu Sasyou

Hirofumi Noda

Ken-ichi Sakai

Astsushi Koiwa

In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

Methods for producing cyclic benzamidine derivatives

The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 &#x212b;, a process for producing them, and a powdery charged preparation for injection containing them.

Carbapenem compound crystals and interjection preparations

Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates

Process for producing stereoisomer of pyrrolidine derivative

Processes for preparing sulfoxides useful as drugs such as acid secretion inhibitors or antiulcer drugs or intermediates for the preparation of drugs in high yields, at high purities, and with safety. Specifically, a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with a peroxoborate salt in the presence of an acid anhydride or a metal catalyst; and a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with an N-halosuccinimide, 1,3-dihalo-5,5-dimethyl-hydantoin or dichloroisocyanuric acid salt in the presence of a base. In said formulae R,is hydrogen, methoxy or difluoromethoxy; R,is methyl or methoxy; R,is 3-methoxypropoxy, methoxy or 2,2,2-trifluoroethoxy; and R,is hydrogen or methyl

Process for the preparation of pyridine derivatives

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Ibaraki, Japan

Akio Kayano