申请人:Vermehren Jan
公开号:US20060004198A1
公开(公告)日:2006-01-05
The invention relates to a preparation process for the compound (I) or a salt thereof
where Q, X*, Y, Z, R, R
1
, R
2
and R
3
are as defined in claim
1
,
which comprises a) monoesterifying a compound (II) where Hal=a halogen atom, giving (III), b) either b1) ammonolysing and phosgenating this compound to give (V) or b2) converting this compound with cyanate into (V) and
c) converting the resulting compound (V) with the aminoheterocycle H
2
N-Het (Het=heterocycle as in (I)) into the compound (I) or a salt thereof. Some compounds (II) and some intermediates (VIII), stabilized with N-heteroaromatic compounds, of the compounds (V) are novel. The compounds (II) can be obtained from the corresponding sulfobenzoic acids by reaction with acid halides of sulfur or phosphorus in nonpolar organic solvents.
本发明涉及化合物 (I) 或其盐的制备工艺
其中 Q、X*、Y、Z、R、R
1
, R
2
和 R
3
如权利要求
1
,
其中包括 a) 单酯化化合物 (II),其中 Hal= 卤素原子,得到 (III), b) b1) 氨解和光合成该化合物,得到 (V) 或 b2) 用氰酸酯将该化合物转化为 (V) 和
c) 将得到的化合物 (V) 与氨基三环 H
2
N-Het(Het=(I)中的杂环)转化为化合物(I)或其盐。化合物(V)的某些化合物(II)和某些中间体(VIII),用 N-杂芳香族化合物稳定,是一种新型化合物。化合物(II)可通过与硫或磷的酸性卤化物在非极性有机溶剂中反应,从相应的磺基苯甲酸中获得。