QIANG YANG,BETH LORSBACH,XIAOYONG LI,GARY ROTH,DAVID E. PODHOREZ
申请号：
ARP140103914
公开号：
AR098108A1
申请日:
2014.10.17
申请国别(地区):
AR
年份:
2016
代理人:
摘要：
3 - (3-chloro-1h-pirazol-1-il) pyridine is produced by 3-hydrazine-pyridine-x2-acrylonitrile-dihydrochlorocyclo, which oxidizes 3 - (3-amine-1h-pirazol-1-il) pyridine and converts the amino compound into a group of chlorine through Sandmeyer reaction. 1. Characteristic 1: preparation process of 3 - (3-chloro-1h-pirazol-1-il) pyridine (5b)；comprising a) treating 3-hydrazinopyridine- × dihydrochloride of formula (1) with acrylonitrile of formula (2) in an aliphatic alcohol C₁₋₄ ₐ ᵘₙₐ ₜₑₘₚₑʳₐₜᵘʳₐ ᵈₑ ₐₚʳₒˣⁱₘₐᵈₐₘₑₙₜₑ ₂₅ºC ₕₐₛₜₐ ₐₚʳₒˣⁱₘₐᵈₐₘₑₙₜₑ ₁₀₀ºC ₑₙ ₚʳₑₛₑₙᶜⁱₐ ᵈₑ ᵘₙ ₐₗᶜóˣⁱᵈₒ ᵈₑ ₘₑₜₐₗ áₗᶜₐₗⁱ C₁₋₄ to obtain 1- (pyridine-3-yl) -4,5-dihydro-1H-pyrazol-1-3-amine of formula (9a)b) treating 1- (pyridin-3-yl) -4,5-dihydro-1H-pyrazol-3-amine of formula (9a) with an oxidant in an organic solvent at a temperature of about 25 ° C to about 100 ° C to supplying 3- (3-amino-1H-pyrazol-1-yl) pyridine of formula (8a)；c) treating 3- (3-amino-1H-pyrazol-1-yl) pyridine of formula (8a) in aqueous hydrochloric acid with sodium nitrite at a temperature of about 0 ° C to about 25 ° C to obtain diazonium salt of formula ( 8b)；and d) treating the diazonium salt of formula (8b) with copper chloride at a temperature of from about 0 ° C to about 25 ° C.Se prepara 3-(3-cloro-1H-pirazol-1-il)piridina mediante la ciclización de 3-hidrazinopiridina- × dihidrocloruro con acrilonitrilo para obtener 1-(piridin-3-il)-4,5-dihidro-1H-pirazol-3-amina, mediante la oxidación de 3-(3-amino-1H-pirazol-1-il)piridina y convirtiendo el grupo amino en un grupo de cloro mediante la reacción de Sandmeyer. Reivindicación 1: Un proceso para preparar 3-(3-cloro-1H-pirazol-1-il)piridina de fórmula (5b), que comprende a) tratar 3-hidrazinopiridina- × dihidrocloruro de fórmula (1) con acrilonitrilo de fórmula (2) en un alcohol alifático C₁₋₄ ₐ ᵘₙₐ ₜₑₘₚₑʳₐₜᵘʳₐ ᵈₑ ₐₚʳₒˣⁱₘₐᵈₐₘₑₙₜₑ ₂₅ºC ₕₐₛₜₐ ₐₚʳₒˣⁱₘₐᵈₐₘₑₙₜₑ ₁₀₀ºC ₑₙ ₚʳₑₛₑₙᶜⁱₐ ᵈₑ ᵘₙ ₐₗᶜóˣⁱᵈₒ ᵈₑ ₘₑₜₐₗ áₗᶜₐₗⁱ C₁₋₄ para obtener 1-(piridina-3-il)-4,5-dihidro-1H-pirazol-1-3-amina de
