Chugai Seiyaku Kabushiki Kaisha

Kaname Tsuzaki

Hitoshi Shimizu

Satoshi Watanabe

Makoto Uehara

Tetsuhiro Mikami

Megumi Ishii

Tadao Michishita

Mitsuhiro Kurita

Akira Hiraide

Masahiro Katoh

Kaichiro Koyama

Koji Oikawa

The present invention provides an E-type crystal of N-demethyl-N-isopropyl-12-methoxy-11-oxo-8,9-anhydroerythromycin A-6,9-hemiacetal fumarate having strong diffraction peaks at diffraction angles (2&#x3b8;) of 5.6&#xb0; and 10.4&#xb0; as measured by powder X-ray diffractometry, which is prepared by treating a C-type crystal of the compound in a mixed solvent of ethyl acetate and water at 20&#xb0; C. to 40&#xb0; C., and a D-type crystal prepared via the E-type crystal. These crystals have a reduced content of residual solvent and high suitability for formulation.

Erythromycin derivative having novel crystal structures and processes for their production

A process for preparing a vitamin D derivative including providing an ultraviolet irradiation apparatus for photochemical reactions, which has an ultraviolet radiation-emitting lamp, an optical system which receives light from the ultraviolet radiation-emitting lamp and emits ultraviolet rays having a specific wavelength, and a quartz rod which receives the ultraviolet rays having the specific wavelength from the optical system and emits the ultraviolet rays, irradiating a solution of a provitamin D derivative with the ultraviolet rays emitted from the quartz rod to cause a photochemical reaction to the provitamin D derivative solution, thereby forming a previtamin D derivative, and subjecting the previtamin D derivative to a thermal isomerization reaction to prepare the vitamin D derivative.

Ultraviolet irradiation apparatus for photochemical reaction and preparation process of vitamin D derivative making use of the same

A method for preparing a fumarate salt of a compound represented by Formula (II):(wherein Rrepresents a hydrogen atom or a lower alkyl group, and Rrepresents a lower alkyl group), which comprises carbamating a compound represented by Formula (I):(wherein Rrepresents a hydrogen atom or a lower alkyl group), removing all carbamate groups from this compound, alkylating the nitrogen atom at the 3'-position of the desosamine ring in the resulting compound to give the compound represented by Formula (II), and converting this compound into a fumarate salt, wherein the compound represented by Formula (I) is carbamated in the presence of a cyclic ether or a carboxylic ester. This method enables efficient preparation of high-quality erythromycin derivatives.

Process for producing erythromycin derivative

Method for preparing purified erythromycin

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Tokyo, Japan

Kaname Tsuzaki