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【结 构 式】

【药物名称】TU-753

【化学名称】17-(2-Methyl-2-propenyl)-4,5alpha-epoxy-3,14-dihydroxy-6,7-didehydroindolo[2',3':6,7]morphinan
      (4bS,8R,8aS,14bR)-7-(2-Methyl-2-propenyl)-6,7,8,9,14,14b-hexahydro-5H-4,8-methano[1]benzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a-diol

【CA登记号】

【 分 子 式 】C26H26N2O3

【 分 子 量 】414.50872

【开发单位】National Institute on Drug Abuse (Originator), National Institutes of Health (Originator), University of Arizona (Originator)

【药理作用】Treatment of Cocaine Dependency, TREATMENT OF POISONING, DRUG ABUSE & DEPENDENCY, Treatment of Substance Dependency, delta-Opioid Antagonists

合成路线1

Noroxymorphindole (III) was prepared by Fischer indole synthesis from noroxymorphone (I) and phenylhydrazine (II) under acidic conditions. Alkylation of (III) with 2-methyl-2-propenyl bromide (IV) in the presence of NaHCO3 in DMF afforded the title compound.

1 McLamore, S.; et al.; Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans on opioid receptor affinity, selectivity, and efficacy. J Med Chem 2001, 44, 9, 1471.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 33927 (1S,5R,13R,17S)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0(1,13).0(5,17).0(7,18)]octadeca-7(18),8,10-trien-14-one C16H17NO4 详情 详情
(II) 11818 Phenyl hydrazine; 1-Phenylhydrazine 100-63-0 C6H8N2 详情 详情
(III) 50974 (1S,2S,13R,21R)-14-oxa-11,22-diazaheptacyclo[13.9.1.0(1,13).0(2,21).0(4,12).0(5,10).0(19,25)]pentacosa-4(12),5,7,9,15(25),16,18-heptaene-2,16-diol C22H20N2O3 详情 详情
(IV) 40015 3-bromo-2-methyl-1-propene 1458-98-6 C4H7Br 详情 详情
Extended Information