A New and Efficient Synthesis of the m-Selective Opioid Antagonist Cyprodime
✍ Scribed by Schmidhammer, Helmut; Krassnig, Roland
- Book ID
- 111907326
- Publisher
- Japan Institute of Heterocyclic Chemistry
- Year
- 1994
- Tongue
- English
- Weight
- 119 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0385-5414
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📜 SIMILAR VOLUMES
## Abstract The preparation of [1‐^3^H]cyprodime (2), which has a specific activity of 31.6 Ci/mmol was carried out by catalytic tritiodehalogenation of 1‐bromocyprodime (3). Bromination of cyprodime was performed by using chloroperoxidase, KBr, and H~2~O~2~.
## Abstract 2‐(3,4‐Dichlorophenyl)‐N‐methyl‐N‐[(1S)‐1‐(3‐isothiocyanatophenyl)‐2‐(1‐pyrrolidinyl)ethyl]acetamide (1, DIPPA) has been previously reported to be an opioid receptor affinity label that produces selective and long‐lasting κ opioid receptor antagonism in mice, High specific activity [^3^
A novel and more efficient synthesis of 14-alkoxy-substituted indolo-and benzofuro-morphinans in three steps starting from either naltrindole (1) or naltriben (2). using methoxymethyl or silyl protecting groups, is reported. The 14-0-alkyl group is introduced at the penultimate step of the procedure