Synthesis And Crystal Structure Determination Of Cyclosporin H

Alexandr Jegorov,Ladislav Cvak,Aleš Husek,Petr Šimek,Anna Heydová,Jan Ondráček,Svetlana Pakhomova,Michal Hušák,Bohumil Kratochvíl,Petr Sedmera,Vladimír Havlíček

COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS（2000）

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摘要

Acid-catalyzed degradation of cyclosporin A was studied in various solvents and products of reaction were monitored by HPLC. Identification of amino acids and their chirality were determined after hydrolysis and derivatization by GC-MS. Cyclosporin H was isolated as the principal product and its structure was determined by X-ray diffraction: Cyclosporin H-diethyl ether-water (1:0.5:1) crystallizes in the monoclinic space group I2 with a = 12.338(2) Angstrom, b = 18.963(2) Angstrom, c = 34.074(3) Angstrom, beta = 96.47(2)degrees, Z = 4, and V = 7921.4(17) Angstrom (3).

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关键词

cyclosporins, conformation analysis, crystal structure determination, X-ray diffraction, hydrolysis, amino acids, peptides, racemization, immunosuppressants

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