MDANIEL KEITH F.,CHEN HUI,JU - SHANLEY JASON P.,GAI YONGHUA,KEMPF DALE J.,GRAMPOVNIK DAVID J.,SUN YING,LIU DONG,WAGAW SABLE H.,ENGSTROM KEN,GRIEME TIM,KU YIYIN,OR YAT SUN
申请号：
ARP120101342
公开号：
AR086181A2
申请日:
2012.04.19
申请国别(地区):
AR
年份:
2013
代理人:
摘要：
Claim 1: method for producing a formula compound (1),Or a pharmaceutically acceptable salt characterized in that it comprises a reaction of a formula compound (2),Where j is - C (o) -；A. alternative heterosexual alternatives； G is - e-r5； E is - n (R3) s (OP) -；P is 2； R5 is optional carbohydrate； each R3 is hydrogen； L is nonexistent； J = 2； k = 2； m = 1； and ---- represents carbon carbon double combination； LG is a discrete group； a formula compound (3),where: each R1 is independently selected from (i) halogen, hydroxy, amino, -CN, -CF3, -N3, -NO2, -OR4, -SR4, -SOR4, -SO2R4, -N (R3) S (O) 2-R4, -N (R3) S (O2) NR3R4, -NR3R4, -C (O) OR4, -C (O) R4, -C (O) NR3R4, or -N (R3) C (O) R4 ； (ii) optionally substituted aryl； (iii) optionally substituted heteroaryl； (iv) optionally substituted heterocycle； (v) optionally substituted carbocycle； or (vi) optionally substituted alkyl, optionally substituted alkenyl, or optionally substituted alkynyl, each containing 0, 1, 2, or 3 heteroatoms selected from O, S, or N；R3 and R4 should be selected independently from the following items in each opportunity: optional tar, optional alquinio or optional tar, each of which has 0, 1, 2 or 3 heteroatoms selected from O, s or N； optional arilo； optional variant； a N is 0, 1, 2, 3 or 4, and CR RSQOE； RSQOE；where R and R together form an aryl ring； to thereby produce a compound of formula (1).Reivindicación 1: Un método para producir un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizada porque comprende el paso de hacer reaccionar un compuesto de fórmula (2), donde, J es -C(O)-； A es heteroarilo opcionalmente sustituido； G es -E-R5； donde E es -N(R3)S(Op)-； p es 2； R5 es carbociclo opcionalmente sustituido； cada R3 es hidrógeno； L se encuentra ausente； j = 2； k = 2； m = 1； y - - - - - denota una unión carbono-carbono doble； y LG es un grupo saliente； con un compuesto de fórmula (3), donde: cada R1 se selecciona independientemente entre (i) halógeno, hi
