Report on a Visit and Conference at the Picatinny Arsenal, Dover New Jersey on July 20-21, 1987 on New Synthetic Approaches to TAT

摘要

First I gave a 1 h 10 min seminar on recent results in TAT synthesis. After discussion of the general synthetic strategies. (Ring synthetic methods, Half synthetic approaches from DAPT Template catalyzed reactions), much attention was paid to the presentation of novel literature in this field found by our group in Bonn, as e.g.: Methyleneimine-Cobaltamine Complexes (cf. Ree et al, Tetrahedron Lett. 1970, 3419); transfer of the TFA method of Dusemund & Schurreit (Arch Pharm ((Weinheim) 319, 826 (1986) on sulfonyl ureas to urea and its alkylation products; As a consequence, the following approaches should be favourably persecuted with great intensity: 1) Condensation experiments of ureas and formaldehyde in TFA; 2) Continuation of TAT approaches with ureas and phosgene; 3) Pursuing the dioxo-tetrazocane approaches via alpha-ureidoalkylation; 4) Search for suitable procedures of selective reductions (avoidance of hydrogenolysis of the carbonyl groups of the latter dioxotetrazocanes; 5) Development of further methods of destructing the methylene bridge in DAPT by simple (& economic) and selective reagents (e.g. BrCN, AgNO2, AgNO3); 6) Further alkylation experiments on DAPTT; 7) Furthermore, clear up the Roumanian Approach; development of better working-up procedures of the 'green complex'; exchange the aniline, e.g. for benzylamine, an easier removable substituent.