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Generated: August 17, 2017

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Title: Aryl fused azapolycyclic compounds
Abstract:Pharmaceutical compositions comprising compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein R.sup.1, R.sup.2, and R.sup.3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
Inventor(s): Coe; Jotham Wadsworth (Niantic, CT), Brooks; Paige Roanne Palmer (North Stonington, CT)
Assignee: Pfizer Inc (New York, NY)
Filing Date:Apr 23, 2002
Application Number:10/131,278
Claims:1. A compound of the formula ##STR26## wherein P is hydrogen, methyl, COOR.sup.16 wherein R.sup.16 is (C.sub.1 -C.sub.6)alkyl, allyl or 2,2,2-trichloroethyl; --C(.dbd.O)NR.sup.5 R.sup.6 ; --C(.dbd.O)H, --C(.dbd.O)(C.sub.1 -C.sub.6)alkyl wherein the alkyl moiety may optionally be substituted with from 1 to 3 halo atoms; --COOCH.sub.2 C.sub.6 H.sub.5, benzyl, t-butoxycarbonyl (t-Boc) or trifluoroacetyl, wherein R.sup.5 and R.sup.6 are each selected, independently, from hydrogen and (C.sub.1 -C.sub.6)alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, N-(C.sub.1 -C.sub.6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine wherein the ring sulfur is replaced with a sulfoxide or sulfone; and R.sup.14 and R.sup.15 are each nitro.

2. A compound according to claim 1 wherein P is selected from the group consisting of --COCF.sub.3, --COCCl.sub.3, --COOCH.sub.2 CCl.sub.3, --COO(C.sub.1 -C.sub.6)alkyl and --COOCH.sub.2 C.sub.6 H.sub.5.

3. A compound according to claim 1 wherein P is t-butoxycarbonyl (t-Boc) or trifluoroacetyl.

4. A compound according to claim 1 wherein P is t-butoxycarbonyl (t-Boc).

5. A compound according to claim 1 wherein P is trifluoroacetyl.

6. A process for preparing a compound of the formula ##STR27## wherein P is hydrogen, methyl, COOR.sup.16 wherein R.sup.16 is (C.sub.1 -C.sub.6)alkyl, allyl or 2,2,2-trichloroethyl; --C(.dbd.O)NR.sup.5 R.sup.6 ; --C(.dbd.O)H, --C(.dbd.O)(C.sub.1 -C.sub.6)alkyl wherein the alkyl moiety may optionally be substituted with from 1 to 3 halo atoms; --COOCH.sub.2 C.sub.6 H.sub.5, benzyl, t-butoxycarbonyl (t-Boc) or trifluoroacetyl, wherein R.sup.5 and R.sup.6 are each selected, independently, from hydrogen and (C.sub.1 -C.sub.6)alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, N-(C.sub.1 -C.sub.6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine ring wherein the ring sulfur is replaced with a sulfoxide or sulfone; and R.sup.14 and R.sup.15 are each nitro; comprising the steps of (i) allowing a compound of the formula ##STR28## wherein P is defined as above; and R.sup.14 and R.sup.15 are both hydrogen to react in the presence of 4 or more equivalents of trifluoromethanesulfonic acid (CF.sub.3 SO.sub.2 OH) and 2 to 3 equivalents of nitric acid.

7. The process according to claim 6 wherein P is selected from the group consisting of --COCF.sub.3, --COCCl.sub.3, --COOCH.sub.2 CCl.sub.3, --COO(C.sub.1 -C.sub.6)alkyl and --COOCH.sub.2 C.sub.6 H.sub.5.

8. A process according to claim 6 wherein P is t-butoxycarbonyl (t-Boc).

9. A process according to claim 6 wherein P is trifluoroacetyl.

10. A process according to claim 6 comprising the prior step of placing a protecting group P on a compound of formula ##STR29##
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