| 主权项 |
1. A process for the synthesis of a compound of Formula IIA by quaternization of a compound of Formula II: wherein, s is 0, 1, 2 or 3; Y— is a pharmaceutically acceptable counterion; each R1, R2, R3, R4, R7 and R8 is independently selected from hydrogen, halogen, —OR20, —SR20, —NR20R21, —C(O)R20, —C(O)OR20, —C(O)NR20R21, —N(R20)C(O)R21, —CF3, —CN, —NO2, —N3, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfonyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl or substituted heterocyclyl; R5, and R6 together with the atoms they are attached form one additional optionally substituted ring; alternatively R2 and R3 together with the carbon they are attached to form a C═X group; wherein each R20 and R21 is independently selected from hydrogen, halogen, —OH, —SH, —NH2, —CF3, —CN, —NO2, —N3, —C(O)OH, —C(O)NH2, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfonyl, aliphatic, substituted aliphatic, aryl or substituted aryl; X is S, O or C(R20)(R21); and, Q is aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl or substituted heterocyclyl; wherein the quaternization process comprises the step of reacting a compound of Formula II with Q-LG in the presence of a base and a solvent, wherein LG is a leaving group; wherein said compound of Formula IIA is insoluble in said solvent. |
