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Process for the preparation of acetylene derivatives having mGluR5 antagonist activity of the compounds, compositions and use
专利权人:
NOVARTIS AG
发明人:
申请号:
ARP120104356
公开号:
AR088921A2
申请日:
2012.11.20
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Process for the preparation of acetylene derivatives that have mgiur5 antagonist activity. Pharmaceutical composition containing same.Claim 1, a process for the preparation of a compound of the formula (1), in which M is 0 OR 1; n is 0 OR 1; and X is Hydrogen, Hydroxy is;And y is Hydrogen; or to form a simple ligation with X or y; r⁰ c₁₋₄ is Hydrogen, alkyl, alkoxy c₁₋₄, trifluoromethyl, halogen, Nitro, cyano -, where is c₁₋₄ coor¹; r¹ alkyl -, or cor²,Where is c₁₋₄ R² Hydrogen or alkyl; and R is cor³ coor³ -, -, - or - conr⁴r⁵ so₂r⁶; where r³ is c₁₋₄ alkyl or cycloalkyl, optionally substituted phenyl c₃₋₇, 1 - or 2 - piridilo tienilo; r⁴ and r⁵,Independently, are Hydrogen or alkyl and alkyl c₁₋₄ r⁶ is c₁₋₄,C₃₋₇ or cycloalkyl optionally substituted phenyl; R is Hydrogen or c₁₋₄ alkyl; and R is Hydrogen or alkyl or c₁₋₄; R and R together form a Group - ch₂ (ch₂) ₚ; where p is 0,1 or 2; in which case one of N and P is different from 0; provided that r⁰ is different from Hydrogen, trifluoromethyl and methoxy when M is 1, N is 0, a is Hydroxy, X and y are both HydrogenIt is cooet R and R and R together form a Group - (ch₂) ₂ - in the form of a Free Base or acid Addition Salt.Characterized in that it comprises the step of: (a) for the production of a compound of the formula (1), in which a is Hydroxy, making a compound of the formula (2), where m, N, r,R and R are as defined in claim 1,A compound of the formula (3), in which r⁰ are as defined in claim 1; or (b) for the production of a compound of the formula (1) which forms a simple ligation with X orAnd dehydrate, a compound of the formula (1) in which a is Hydroxy, and retrieve the resulting Compound of the formula (1), in the form of a Free Base or acid Addition Salt.Proceso para la preparación de derivados de acetileno que tienen actividad antagonista mGIuR5. Composición farmacéutica que lo comprende. Reivindicación 1: Un proceso para la preparación de un compuesto de la fórmula (1), en la que: m es 0 ó 1; n es 0 ó 1
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