纳多洛尔合成研究的改进  

Improvement on Synthesis of Nadolol

作　　者：蒋忠良[1] 王娟[1] 何继颖[1] 

机构地区：[1]同济大学理学院化学系,上海200092

出　　处：《精细与专用化学品》2007年第7期15-16,14,共3页Fine and Specialty Chemicals

摘　　要：以α-萘酚为原料，经过还原、酰化、氧化、醚化和胺化等一系列步骤制备了纳多洛尔。5，8-二氢-1-萘酚的收率为93．9％，熔点68～69℃；顺-5，6，7，8-四氢-6，7-二羟基．1．萘酚的收率为54．3％，熔点181—183℃；顺-5，6，7，8-四氢巧，7-二羟基-1-环氧丙基萘酚的收率为86．9％；纳多洛尔的收率为77％，熔点121—123℃。并用HNMR对顺-5，6，7，8-四氢击，7-二羟基-1-萘酚、顺-5，6，7，8-四氢-6，7-二羟基-1-环氧丙基萘酚和纳多洛尔进行了确证。Using α-naphthol as raw material, nadolol was synthesized through reaction steps comprising of reduction, acylation, oxidation, etherification and amination. The yields and melting points of two following intermediates 5,8-dihydrogen-1-naphthol （ 1 ） and cis-5,6,7,8-tetrahydrogen-6,7-dihydroxy-l-naphthol （ 2 ） were 93.9% , 68 - 69℃ ; and 54. 3% , 181 - 183℃ respectively. The yield of cis-5,6,7,8-tetrahydrogen-6,7-dihydroxy-l-epoxypropylnaphthol （3） was 86.9% , and the yield and reciting point of final product nadolol were 77% and 121 - 123℃ respectively. The compounds of （2） , （3） and （4） were confirmed by 1HNMR.

关 键 词：纳多洛尔 Α-萘酚 5 8-二氢-1-萘酚 Β-受体阻滞药 

分 类 号：TQ463.53[化学工程—制药化工]