Nous avons prkctdemment montrk [l] [2] que le traitement des azadilnes 1 par I'ammoniac ou les amines primaires (SchBma 1) conduit a des pyrazinecarbonitriles ou pyrazinecarboxylates de mtthyle ortho-aminks ou a des iminopyrazine 3. Ces pyrazines sont des intermediaires utiles dans l'klaboration de squelettes ptkridines substituks de
The process development and improvements for route selection, adapted to large scale for the pilot-scale preparation of SL65.0102-10, an N-diazabicyclo[2.2.2]-octylmethyl benzamide, a 5-HT 3 and 5-HT 4 receptor active ligand for the treatment of neurological disorders such as cognition impairment, are described in this article. Notable steps and enhancements are compared to the original route, including the improvement of a chiral epoxide synthesis by shortening the number of chemical steps, the deprotection of a quaternary ammonium salt, and the redesign of the final amidification coupling to avoid chromatography.
'lerr-Amino Effect' on Acidic Treatment of (Pyrrolidin-1-y1)azadienesThe behaviour of 4-morpholino-and 4-(pyrrolidin-l -yl)-2-aza-I ,3-diene-l, I-dicarbonitriles 3, and 4 and 10, respectively, in acidic medium is described. The former gives with HBr/AcOH 3-bromopyrazine-2-carbonitrile 6. triles ou imidazole-2-carbonitriles suivant la nature de X. Le fragment de base R,N, prksente dans l'azadiene, n'influence g d r e que la vitesse de formation de l'intermediaire 2, la nature des produits finaux n'en ktant pas affectke.Nous decrirons dans ce memoire I'action des acides sur ces m2mes azadienes et le r61e important jouC par le substituant R,N dans un tel milieu.
Reaction of the ester (Ia) and the nitrile (Ib) with a series of nitrogen compounds leads to formation of N‐heterocycles of type (V)‐(VII), (IX) and (XI).
The title compounds (III) and (V) furnish, by a (1,5)‐H shift, the heterocyclic systems (IV) and (VI), resp.; the latter loose HCN spontaneously to give (VII).
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