| 主权项 |
1. A method for synthesizing a cycloalkanyl[b]indole, comprising
(a) combining, in a single reaction,
(i) a compound of Formula I, (ii) a compound of Formula II or III, and (iii) a coupling partner; and (b) adding an acid catalyst thereby producing a compound of Formula Va, Vb, Vc or Vd wherein, X is NR1, wherein R1 is hydrogen, or alkyl each Y is C; at least two of the three dashed bonds are present; each R2 is the same or different and is independently selected from the group of hydrogen, a halogen, alkyl, alkoxy, aryl, —NHR7, —OR8, —O-aryl, —NR8R9, —NR8-aryl, —C(O)R8, —CO2R8, —C(O)NR8R9, —C(O)aryl, —C(O)NR8aryl, —C(O) Het, —C(O)NHR7Het, —S(O)2NR8R9, —S(O)2N R8aryl, and cyano; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl, —NHR7, —OR8, —O-aryl, —NR8R9, —NR8-aryl, —C(O)NR8R9, —C(O)aryl, —C(O)NR8aryl, —C(O) Het, —C(O)NHR7Het, —S(O)2NR8R9, —S(O)2N R8aryl, and cyano, or R3 and R4 together form a C4-6 cycoalkyl; R5 is alkyl; each R6 is the same or different and is independently selected from the group of hydrogen, alkyl, cycloalkyl, and aryl; each R7 is the same or different and is independently selected from an alkylene, cycloalkylene, alkenylene, cycloalkenylene or alkynylene group; each of R8 and R9 are the same or different and are independently selected from the group of hydrogen, an alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, —R7cycloalkyl, —R7OH, —R7(OR7)w, or —R7NR10R11 group; each of R10 and R11 are the same or different and are independently selected from the group of an alkyl, cycloalkyl, alkenyl, cycloalkenyl, or alkynyl group; p is selected from 0, 1, or 2; q is selected from 0, 1, or 2; w is 1-10. |
