close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2005
Pyridine derivatives
R 0380
Functionalization at Position 3 of the Phenyl Ring of the Potent mGluR5 NoncomAntagonists MPEP. — MPEP analogues (V) are synthesized by a modified
25- 143 petitive
Sonogashira reaction involving in situ desilylation of acetylene precursor (III) and subsequent palladium cross-coupling with aryl bromides (IV). The same cross coupling
using heteroaryl bromide (VI) yields key intermediate (VII). Stille reaction between
(VII) and trialkyl stannanes provides analogues (VIII). The results obtained show the
limitation in the choice of a functional group at position 3; only analogues (V) retain
activity. Pyridine analogues (VIII) display good binding for mGluR5, despite a lack of
activity in the functional receptor assay. — (ALAGILLE, D.; BALDWIN, R. M.;
ROTH, B. L.; WROBLEWSKI, J. T.; GRAJKOWSKA, E.; TAMAGNAN*, G. D.;
Bioorg. Med. Chem. Lett. 15 (2005) 4, 945-949; Dep. Psychiatr., Yale Univ., West
Haven, CT 06516, USA; Eng.) — H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
20 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа