Process for preparing oxazoles by condensation of aromatic aldehyde with alpha cetoximas for n - Oxides and subsequent reaction with activated acid derivatives

摘要

Industrial property 1: a process for the preparation of formula compounds (4), including the conversion of aromatic aldehydes from the formula (1), the use of alpha hexachlorobenzene (2), wherein R1 is h, C1-6, F, Cl, Br, I, o-tar c0-8-h, CF3, ocf3, ScF3, sF5, ocf2-chf2, arilo C6-10, o-arilo C6-10, o-oc-4-arilo c6-no9, coo9, Conr10r11, SH or n10r11, where arilo is not replaced or monkey,Di-o tristitude co F, Cl, Br, I, C1-4, o-tar C1-4 or CF3; wherein R9 is h, Li, Na, K, 1 / 2 Ca, unreplaced ammonium ion or monkey,Di - or carbon trifluoride C1-4 tar or c1-8 tar; each R10 and R11 is an independent h, C1-5 tar, phenyl or ch2-phenyl, phenyl is not substituted or monkey,6-6-6-6, c6-6-6 or c6-6-6, c6-6-6-6 c1-4-arilo C6-10, NO2, coor9, Conr10r11, SH or n10r11, where arilo is not replaced or monkey,di- or trisubstituted with F, Cl, Br, I, C1-4alkyl, O-C1-4alkyl or CF3; where each of R9, R10 and R11 is as defined above; R3 is H, C1-6 alkyl, F, Cl, Br, I, O-C0-8-H-alkylene, CF3, OCF3, SCF3, SF5, OCF2-CHF2, C6-10 aryl, C6-10 O-aryl, O-C1-4-alkylene-C6-10 aryl, NO2, COOR9, CONR10R11, SH or NR10R11, where the aryl is unsubstituted or mono-,di- or trisubstituted with F, Cl, Br, I, C1-4alkyl, O-C1-4alkyl or CF3; where each of R9, R10 and R11 is as defined above; W is CH, N, if o = 1, W is O, S, NR12, if o = 0; o is 0 or 1; R12 is H, C1-6alkyl, C1-6alkylenephenyl, phenyl; R4 is H, C1-8 alkyl, C3-8 cycloalkyl, C1-3 alkylene-C3-8 cycloalkyl, phenyl, C1-3 alkylene phenyl, C5-6 heteroaryl, C1-3 alkylene-C5-6 heteroaryl or C1-3 alkyl which is wholly or partially substituted with F or is COOR9, CONR10R11; where each of R9, R10 and R11 is as defined above; each of R5 and R6 is independently is H, C1-8 alkyl, F, Cl, Br, I, O-C0-8-alkylene, C6-10 O-aryl,O-c1-4-arilo C6-10, cour9, conr10 R11, SH or nr10 R11, where each R9, R10 and R11 is consistent with the above definition; or R5 and R6 together are C4-5 tar, one CH2 group can be replaced by O, s, NH, n-ch3 or n-bencilo; R7 is h or c1-8 tar; and each R1 has an acid in the formula, 3333c3-33c3-333c3, from a variety of 4-so2-o3s-c6h4-p-ch3,In formula (4), each R1, R2, R3, R4, R5, R6 and X2 is defined as above, and X3 is Cl, Br, ch3so3, cf3so3, c6h5so3 or p-ch3-c6h4-so3 and N2 is 0 or 1.