On January 10, 1990, Comte, Marie Therese; Gueremy, Claude; Malleron, Jean Luc; Mignani, Serge; Peyronel, Jean Francois; Truchon, Alain published a patent.Recommanded Product: 58142-46-4 The title of the patent was Preparation and formulation of (aza)naphthalenesultam derivatives as serotoninergic antagonists. And the patent contained the following:
Title compounds I [R1 = 4-(hetero)aryl-substituted 1,2,3,6-tetrahydro-1-pyridyl, 1-piperazinyl, or piperidino; R2, R3 = H, halo, R4 = H; or R2 = R4 = H, R3 = halo, AcNH; or R2 = R3 = H, R4 = halo, all with X = CH; or R2 = R3 = R4 = H, X = N; Z = (un)substituted alkylene; various provisos] were prepared as serotonergic 5-HT2 receptor antagonists (no data). Thus, N-alkylation of 1,8-naphthosultam by Br(CH2)3Cl using NaH in DMF gave the N-(3-chloropropyl) derivative, which reacted with 1-(4-fluorophenyl)piperazine in PhMe containing Et3N to give (piperazinylpropyl)naphthoisothiazole derivative II. Three formulations and 61 syntheses are given. The IC50 of I for displacement of [3H]-ketanserin from 5-HT receptors are said to be generally <25 nM. The experimental process involved the reaction of 4-Bromo-5-nitroisoquinoline(cas: 58142-46-4).Recommanded Product: 58142-46-4
The Article related to naphthalenesultam preparation serotoninergic antagonist, naphthoisothiazole preparation 5ht antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 58142-46-4
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem