Title:
ONE-STEP PREPARATION OF DIRITHROMYCIN
Document Type and Number:
Japanese Patent JP3197957
Kind Code:
B2
Abstract:
PURPOSE: To easily obtain a compd. in high yield in a single reaction chamber by dissolving an acetal in an aq. acetonitrile, hydrolyzing the mixture in the presence of an acid catalyst, and then allowing the product to react with erythoromycylamine.
CONSTITUTION: An acetal expressed by the formula (R1, R2 are a 1 to 6C alkyl or bonded to form 2-CH2-CH2-, etc., or may be bonded to the structural body to form 5- to 7-membered ring), preferably 2-(2-methoxyethoxy)acetaldehyde diethylacetal, is dissolved in an aq. acetonitrile (preferably having about 4% water content) and hydrolyzed for a specified time in the presence of an acid catalyst (preferably p-toluenesulfonic acid). Then erythromycylamine is added to react to obtain the objective compd. The objective compd. is, for example, 9-deoxo-11-deoxy-9,11-{imino[2-(2-methoxyethoxy)ethylidene]oxy}-(9S)- erythromycin.
Inventors:
John McNail McGill
Application Number:
JP26002192A
Publication Date:
August 13, 2001
Filing Date:
September 29, 1992
Export Citation:
Assignee:
ELI LILLY AND COMPANY
International Classes:
C07H1/00; C07H17/08; (IPC1-7): C07H17/08; C07H1/00
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)