Patent ID: 8309722

Claim:
A method for preparing a compound of Formula 2F wherein: (i) k is 1; (ii) m is 1; (iii) n is 1; (iv) B is a selected from the group consisting of C 1-6 alkoxycarbonyl, arylmethoxycarbonyl, triphenylmethyl, phenylcarbonyl, benzyl, 1-arene sulfonyl and toluene sulfonyl; or B is a compound of the formula: wherein: a) Z is C 1-6 alkyl, aryl, C 1-6 alkylaryl or —OR wherein R is C 1-6 alkyl, aryl, arylC 1-6 alkyl or heteroarylC 1-6 alkyl; b) P is —C(O)—, —C(O)O— or —S(O) 2 —; (v) R 5 is H or C 1 -C 4 alkyl; (vi) R 7 , R 8 and R 9 are independently H, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 heterocycloalkyl, hydroxy, C 1 -C 6 alkoxy, nitro, halo, haloC 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, heteroaryl or heteroarylC 1 -C 6 alkyl; and (vii) —X—Y— is (R′)N—CH 2 — or —(R′)N—C(O)—, wherein R′ is H or C 1-4 alkyl, in free base or acid addition salt form, which method comprises the step of reacting a compound of Formula 2E: wherein: (i) k is 1; (ii) m is 1; (iii) n is 1; (iv) A is Cl, Br, F or I; (v) B is selected from the group consisting of C 1-6 alkoxycarbonyl, arylmethoxycarbonyl, triphenylmethyl, phenylcarbonyl, benzyl, 1-arene sulfonyl and toluene sulfonyl; or B is a compound of the formula: wherein: a) Z is C 1-6 alkyl, aryl, C 1-6 alkylaryl or —OR wherein R is C 1-6 alkyl, aryl, arylC 1-6 alkyl or heteroarylC 1-6 alkyl; b) P is —C(O)—, —C(O)O— or —S(O) 2 —; (vi) R 5 is H or C 1 -C 4 alkyl; (vii) R 7 , R 8 and R 9 are independently H, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 heterocycloalkyl, hydroxy, C 1 -C 6 alkoxy, nitro, halo, haloC 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, heteroaryl or heteroarylC 1 -C 6 alkyl; and (viii) X—Y— is a H(R′)N—CH 2 — or H(R′)N—C(O)—, wherein R′ is H or C 1 -C 4 alkyl, in free base or acid addition salt form, with (a) a copper catalyst; and (b) a base.