| 摘要 |
Preparation of tertiary nitrite-substituted aromatic compound final products (I). Preparation of tertiary nitrite-substituted aromatic compound final products of formula (I) comprises treating an aromatic compound of formula (II) with a secondary nitrile of compound (III) in the presence of a base with a pKa of 17-30, provided that the difference in pKa numerical values between the base and (III) is no more than 6 in an aprotic solvent with a dielectric constant (eta ) of less than 20 and at 0-120[deg]C. [Image] W 1-W 5C, N, O, S(=O) k or absent, provided that only one is absent, no more than one is O or S(=O) k optionally together with one N in each case and no more than four are N where only N is present; R 1-R 5(a) absent when W 1-W 5 is O or S(=O) k, (b) when W 1-W 5 is C = H, Cl, Br or I, N(R 1 2) 2, SR 1 2, OR 1 2, 1-6C alkyl (substituted by 0-3 R 9, N(R 12) 2, SR 12 or OR 12), 2-6C alkenyl substituted by 0-3 R 9, 3-6C alkynyl substituted by 0-3 R 9, 3-14C carbocyclic ring system substituted by 0-3 R 9 or 0-3 R 10, heterocyclic ring system chosen from furanyl, thienyl, pyrrolyl, imidazolyl, pyridyl, pyrazolyl, pyrimidinyl, benzofuranyl, benzothienyl, indolyl, benzimidazolyl, tetrahydroisoquinolinyl, benzotriazolyl or thiazolyl (all substituted by 0-2 R 10) or, together, form a fused 5-6-membered ring optionally substituted on any aliphatic C atom by Cl, Br or I, 1-4C alkyl, 1-4C alkoxy or NR 15R 16, or (c) when W 1-W 5 = N = phenyl, benzyl, phenethyl, phenoxy, 1-4C alkyl, 1-4C alkoxy, 3-6C cycloalkyl, 3-6C cycloalkylmethyl, CH 2NR 15R 16, NR 15R 16, 2-6C alkoxyalkyl or C(R 16) =N(OR 16); and R 6, R 7N(R 12) 2, 1-6C alkyl, 2-6C alkenyl or 3-6C alkynyl (all substituted by 0-3 R 9), N(R 12) 2, SR 12, OR 12, 3-14C carbocyclic ring (substituted by 0-3 R 9 or 0-3 R 10) or heterocyclic ring system chosen from furanyl, thienyl, pyrrolyl, imidazolyl, tetrahydropyranyl, pyridyl, piperidinyl, pyrazolyl, pyrimidinyl, benzofuranyl, benzothienyl, indolyl, benzimidazolyl, tetrahydroisoquinolinyl, benzotriazolyl, thiazolyl (all substituted by 0-2 R 10) or, taken together, form 3-14C carbocyclic ring system (substituted by 0-3 R 9 or 0-3 R 10), phenyl, 1- or 2-naphthyl (substituted by 0-3 R 9 or 0-3 R 10) or heterocyclic ring system chosen from furanyl, thienyl, pyrrolyl, imidazolyl, tetrahydropyranyl, pyridyl, piperidinyl, pyrazolyl, pyrimidinyl, benzofuranyl, benzothienyl, indolyl, benzimidazolyl, tetrahydroisoquinolinyl, benzotriazolyl, thiazolyl (all substituted by 0-2 R 10). |
