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纳多洛尔合成研究的改进 被引量:1

Improvement on Synthesis of Nadolol
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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.
出处 《精细与专用化学品》 CAS 2007年第7期15-16,14,共3页 Fine and Specialty Chemicals
关键词 纳多洛尔 Α-萘酚 5 8-二氢-1-萘酚 Β-受体阻滞药 nodolol α-naphthol 5,8-dihydrogen-1 -naphthol β-aceptor blocker
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  • 1徐济民.纳多洛尔的药理和临床应用[J].医药简讯(上海),1990,10(4):19-22. 被引量:1
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  • 4[4]Narayanan Venkatachala L.Tetrahydro-cyclopropa[8] naphthalenes[P].US3969392,1976-07-13

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