GERARD J. TANOURY,YOUNG CHUN JUNG,DEREK MAGDZIAK,ADAM LOOKER
申请号：
ARP120102438
公开号：
AR087069A1
申请日:
2012.07.05
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
1. The processing technology and the intermediate are used to produce useful compounds as inhibitors of 1500 anu (JAK). These compounds help to treat diseases such as autoimmune diseases (allergies, asthma),transplant rejection, leukemia, lymphomas, polycythemia, essential thrombocythemia, myelofibrosis. Claim 1: A process for preparing a compound of formula (1) or a pharmaceutically acceptable salt thereof, characterized in that: R¹ is -H, -Cl or -F； R² is -H or -F； R³ is -aliphatic C₁₋₄ optionally substituted with 1-5 occurrences of R⁵；R⁴ is -Cquilalkyl optionally substituted with 1-3 occurrences of R⁵；O r 3 and r830808 together form a saturated carbon o r heterocyclic ring composed of 3-7 selective members, which is replaced by 1-5 of r83099；Each r83099 should be selected independently between halogen-oc832323；-Oh, no, 832222,-NH832222,-SH, -SCH₃,-NHCH₃,-CN o alif tico C insustituido o dos grupos Rtogether with the carbon to which they are attached, they form a cyclopropyl ring； R⁶ is -H or unsubstituted C₁₋₂ alkyl； and R⁷ is a -CH₂CR₃ or - (CH₂) ₂CR₃ where each R is independently -H or -F； comprising the steps of: i) reacting a compound of the formula (2) with a hydrochloride salt of a compound of the formula (3) in the presence of water, an organic solvent, a base and a transition metal catalyst to generate a compound of formula (1).La presente se refiere a procesos e intermediarios para la preparación de los compuestos útiles como inhibidores de las quinasas Janus (JAK). Estos compuestos son útiles en el tratamiento de dolencias tales como las enfermedades autoinmunes (alergia, asma), rechazo de transplantes, leucemia, linfomas, policitemia, trombocitemia esencial, mielofibrosis. Reivindicación 1: Un proceso para preparar un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, caracterizada porque: R¹ es -H, -Cl o -F； R² es -H o -F； R³ es -alifático C₁₋₄ opcionalmente sustituido con 1 - 5 ocurrencias de R⁵； R⁴ es -alquil C₁₋₂ opcionalme
