Efficient and green clarithromycin intermediate synthesis process

• Main Authors: ZHANG GENGZHEN, WANG FENG
• Format: Patent
• Language: Chinese; English
• Published: 31.05.2017
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; DERIVATIVES THEREOF; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SUGARS; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

The invention discloses an efficient and green clarithromycin intermediate synthesis process. Erythrocin A-9-oxime is dissolved in an organic solvent; a strong acid catalyst is used; an etherifying agent is added; reaction is performed for 0.25 to 3h; then, a silanization protecting group and an alkylation catalyst are added; temperature rise is performed for regulating pH; etherification reaction is performed; then, water is added; reaction is terminated; the pH is regulated; water washing layering and concentration are performed to obtain a clarithromycin intermediate compound. The synthesis process has the advantages that the use of alkylation and etherifying agents can be reduced; the reaction time is reduced; the conversation rate is improved; green and environment-friendly effects are achieved; the recovery is easy. 本发明公开了种高效绿色克拉霉素中间体合成工艺。红霉素A-9-肟溶于有机溶剂中采用强酸催化剂加入醚化剂反应小时，再加入硅烷化保护基和烷化催化剂升温调节pH进行醚化反应，然后加水终止反应，调节pH到，水洗分层浓缩得到作为克拉霉素中间体的化合物。本发明能够减少烷化和醚化剂的使用，减少反应时间，提高转化率，绿色环保，易于回收。