𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis of 2H- and 3H-labeled N-cyclopropylmethyl-7α-[(R)-1-hydroxy-1-methyl-3-(2thienyl)-propyl]-6,14-endoethano-6,7,8,14-tetrahydro nororipavine

✍ Scribed by Bo Wu; Lanfu Chen; Jingyan Wang; Chunhe Liu; He Liu; Bohua Zhong

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
142 KB
Volume
48
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

A procedure for deuterium and tritium labeling of the titled compound, an analgesic agent, was developed. A secondary amine intermediate was acylated to an acylamide, then the carbonyl function was reduced by LiAlD 4 to yield the tertiary amine. In the tritium-labeled synthesis, the process utilized a bromo-substituted precursor, which was subsequently reduced with 3 H 2 in the presence of a Pd/C catalyst. The labeled compounds were successfully applied in pharmacokinetic and pharmacological studies.

📜 SIMILAR VOLUMES

Polycyclic N-Heterocyclic compounds. 50.
Polycyclic N-Heterocyclic compounds. 50. Synthesis and pharmacological evaluation of 2,3,6,7-Tetrahydrothieno[2,3-H]-imidazo[2,1-f][1,6]naphthyridines,3,4,7,8-Tetrahydro-2H-thieno-[2,3-h]pyrimido[2,1-f][1,6]naphthyridines and their precursor
✍ Kenji Sasaki; Abu Shara S. Rouf; Takashi Hirota; Naoki Nakaya 📂 Article 📅 1999 🏛 Journal of Heterocyclic Chemistry 🌐 English ⚖ 379 KB

## Abstract Some novel 5‐hydroxyalkylamino‐1,2‐dihydrothieno[2,3‐__h__][1,6]naphthyridines were prepared by the reaction of 5‐chloro‐1,2‐dihydrothieno[2,3‐__h__][1,6]naphthyridine derivatives with some aminoalcohols in the presence of base. These derivatives were cyclized to the corresponding imida