Dirithromycin industrial production method

The invention provides a dirithromycin industrial production method. The method comprises the following steps: 1) by using erythromycin thiocyanate (DHMSM1) as an initial raw material, carrying out condensation with hydroxylamine hydrochloride to obtain an intermediate erythromycin oxime (DHMS01), c...

Full description

Saved in:
Bibliographic Details
Main Authors YAN JIAXIAO, HU MENGQI, JIANG WEI
Format Patent
LanguageChinese
English
Published 07.12.2016
Subjects
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
Online AccessGet full text

Cover

More Information
Summary:The invention provides a dirithromycin industrial production method. The method comprises the following steps: 1) by using erythromycin thiocyanate (DHMSM1) as an initial raw material, carrying out condensation with hydroxylamine hydrochloride to obtain an intermediate erythromycin oxime (DHMS01), carrying out reduction with reduction reagents titanium trichloride and sodium borohydride to obtain an intermediate erythromycin amine (DHMS02), carrying out condensation with dirithromycin side chain (DHMSSM22-(2-methoxyethoxy)acetaldehyde) to obtain a dirithromycin crude product, and carrying out recrystallization and crystal transformation to obtain the finished product. No special reaction conditions are required in the synthesis process. The purity is greater than 99.5%, the ee value can reach 100%, the single impurity content is less than 0.1%, and the dirithromycin satisfies the requirements for medicinal active pharmaceutical ingredients. 本发明提供了种地红霉素工业化生产方法，该方法包括以下步骤：1）以硫氰酸红霉素(DHMSSM1)为起始原料，与盐酸羟胺缩合得到中间体红霉素肟
Bibliography:Application Number: CN20161625048