| 主权项 |
1. A process for preparing a compound of formula (II):or a salt thereof;
from a compound of formula (I):or a salt thereof;wherein:
R1 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, haloalkyl, —OR16, —C(O)R16, —CO2R16, —SO2R16, —C(O)N(R17)(R17), —[C(R16)2]q—R16, —[(W)—N(R17)C(O)]qR16, —[(W)—C(O)]R16, —[(W)—C(O)O]R16, —[(W)—OC(O)]qR16, —[(W)—SO2]qR16, —[(W)—N(R17)SO2]R16, —[(W)—C(O)N(R17)]qR17, [(W)—O]qR16, —[(W)—N(R17)]qR16, or —[(W)—S]qR16; wherein W is a diradical and q is 1, 2, 3, 4, 5, or 6; each R2 and R3 is, independently, H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, haloalkyl, halo, —OR16, —OR16, —N(R17)2, or —SR16, or R2 and R3 taken together form a double bond or form a group wherein Z is NR17, O, or C(R18)2; R4 is independently H, halo, —OR16, —N(R17)2, or —SR16; each R5 and R6, is, independently, H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, halo, —OR16, —N(R17)2, or —SR16; or R5 and R6 taken together with the carbon to which they are bonded form C═O, C═S, C═N—OR17, C═N—R17, C═N—N(R17)2, or form an optionally substituted 3-8 membered ring; each R7, R8, R9, R10, R11, R12 and R13 is, independently, H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, halo, —OR16, —N(R17)2, or —SR16; or R10 and R11 taken together, or R11 and R12 taken together, form a double bond or form a group wherein Z is NR17, O, or C(R18)2; each R14 and R15 is, independently, H, halo, —OR16, —N(R17)2, or —SR16; or R14 and R15 taken together with the carbon to which they are bonded form C═O or C═S; X is a bond or the group —C(R19)2—; wherein each R19 is, independently, H, alkyl, aralkyl, halo, —CN, —OR16, or —N(R17)2; R16 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl or —[C(R20)2]p—R21 wherein p is 0-6; or any two occurrences of R16 on the same substituent are taken together to form a 4-8 membered optionally substituted ring; R17 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, —C(═O)R20, —C(═O)OR20, —SO2R20, —C(═O)N(R20)2, or —[C(R20)2]p—R21 wherein p is 0-6; or any two occurrences of R17 on the same substituent are taken together to form a 4-8 membered optionally substituted ring; R18 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl, halo, —CN, —OR20, —OSi(R20)3, —C(═O)R20, —C(═O)OR20, —SO2R20 or —C(═O)N(R20)2; R20 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, or heteroaralkyl; or any two occurrences of R20 on the same substituent are taken together to form a 4-8 membered optionally substituted ring; R21 is —OR22, —N(R22)C(═O)R22, —N(R22)C(═O)OR22, —N(R22)S2(R22), —C(═O)R22N(R22)2, —OC(═O)R22N(R22)(R22), —SO2N(R22)(R22), —N(R22)(R22), —C(═O)OR22, —C(═O)N(OH)(R22), —OS(O)2OR22, —S(O)2OR22, —OP(═O)(OR22)(OR22), —N(R22)P(O)(OR22)(OR22), or —P(═O)(OR22)(OR22); and R22 is H, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocycloalkyl, aralkyl, heteroaryl, heteroaralkyl; or any two occurrences of R22 on the same substituent are taken together to form a 4-8 membered optionally substituted ring;
said process comprising contacting a compound of formula (I) or a salt thereof, an amino donor molecule, and an omega amine transaminase enzyme in a solution to provide a compound of formula (II) or a salt thereof. |
