ChemInform Abstract: Naphthosultam Derivatives: A New Class of Potent and Selective 5‐HT2 Antagonists.

Abstract

Naphthosultam Derivatives: A New Class of Potent and Selective 5-HT2 Antagonists.-A series of 2-aminoalkyl-1,8-naphthosultams such as (V) is prepared by consecutive coupling of 1,8-naphthosultam (I) with the dihalides (II) and the corresponding secondary amines (IV). Among these, the derivative (Ve) shows the highest 5-HT2 receptor affinity. -(MALLERON, J.-L.; COMTE, M.-T.; GUEREMY, C.; PEYRONEL, J. F.; TRUCHON, A.; BLANCHARD, J. C.; DOBLE, A.; PIOT, O.; ZUNDEL, J.-L.; HUON, C.; MARTIN, B.; MOUTON, P.; VIROULAUD, A.; ALLAM, D.; BETSCHART, J.; J. Med. Chem. 34 (1991) 8, 2477-2483; Dep. Chim. Pharm. Biol., Centre Rech. Vitry Alfortville Rhone-PoulencRorer, 94403 Vitry-sur-Seine, Fr.; EN)

Current radiosynthesis strategies for 5‐HT2A receptor PET tracers

“…Radiosynthesis of [ 18 F]fananserin (a) Br(CH 2 ) 3 Cl; (b) HN(CH 2 CH 2 OH) 2 , CBr 4 , Ph 3 P; (c) kryptofix 2.2.2., 18 F − , K 2 CO 3 ; (d) Pd/C, H 3 PO 2 ; and (e) NaHCO 3 …”