Procedures for preparing N - pyridazinones oxazolidinones through a Cross coupling reaction catalyzed by Copper

摘要

The procedure of preparing ammonium octanoate by cross coupling reaction catalyzed by copper was described. A compound used in the manufacture of CETP inhibitors. 1. Claim 1: a program for preparing a compound formula (1),Among them, R1 is a partially saturated, saturated or completely unsaturated linear carbon (C1-4) or branch, in which the carbon other than the connected carbon may be replaced by a non oxygen atom, Sulfur and nitrogen, these carbon atoms are optional singletons,Di-o tri - is replaced by halide independently. This kind of carbon can be replaced by Oxo or hydroxi in a single time, oxo in a single time, oxo in a single time or oxo in a single time, or R1 is a 3-5 partially saturated ring, Completely saturated or completely unsaturated, or completely unsaturated, there is an optional heteroatom between oxygen, sulfur and nitrogen, in which R1 ring is an optional monkey,It is independent of halogenated and propoxy (C1-6) sulfur dioxide-o trifluoride,Nitric acid, tar (C1-4) oxycarbide; R2 is hydrogen, tar (C1-4),Bicycle (C3-6),alquenilo (C2-6)Penicillin (c2-6),alcoxi (C1-4)2. Alcox (C1-4) - tar (C1-4);Instead of phenyl, Alcoy (C1-6) or oy is a protective group of hydroxyl, halogen and hydrocarbon (C1-4),alquenilo (C2-6)Penicillin (c2-6),Alcox (c1-49, alcoxi (C1-4) - tar (C1-4),Trifluoroide; nitro, carboxy (C1-4),alcoxi (C1-4) -carbonilo carbonilo o ciano o bencilo con el resto fenilo del bencilo sustituido opcionalmente con alcoxi (C1-6) u OY en el que Y es un grupo protector de hidroxi hal geno alquilo (C1-4)alquenilo (C2-6)Penicillin (c2-6),Alcox (C1-4) - tar (C1-4),3. Trifluoroamide, nitro, calcium carbonate (C1-4),(C1-4) alkoxy -carbonyl, carbonyl or cyano; where Ar is Ar is an aromatic or heteroaromatic hydrocarbon residue selected from the group consisting of phenyl, naphthyl, pyridyl, thiophenyl, furanyl, pyrrolyl, and pyrimidyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, pyrazolyl, pyrazinyl, pyridazinyl each of which it may be optionally substituted with one or more, preferably one or two, substituents independently selected from the group consisting of halogen, hydroxyl, (C1-4) alkyl,alquenilo (C2-6)Penicillin (c2-6),alcoxi (C1-4)Alcox (C1-4) - tar (C1-4),Sulfur trifluoride (CF3),amino amido iminas nitro carbo-alcoxi (C1-4)alcoxi (C1-4) -carbonilo carbonilos (cetonas y aldeh dos)Cyanogen; characterized in that it includes the reaction of a compound formula (2),Among them, R4 is a partially saturated, saturated or unsaturated linear carbon (C1-4) or branch, in which the carbon other than the connecting carbon may be replaced by the heteroatom without oxygen, Sulfur and nitrogen, these carbon atoms are optional monkeys,Di-o tri - is replaced by halide independently, such carbon can choose to use oxo or hydroxi instead of monomer, such sulfur can choose monomer or monomer or monomer - instead of oxo, such nitrogen can choose monomer or monomer - instead of oxo, or R1 is a 3-5-part saturated, fully saturated or Completely unsaturated, selective heteroatoms are selected from oxygen, sulfur and nitrogen, among which R1 ring is the optional monkey,It is independent of halogenated and propoxy (C1-6) sulfur dioxide-o trifluoride,Nitro, tar (C1-4) oxycarbide; R5 is hydrogen, tar (C1-4),Bicycle (C3-6),alquenilo (C2-6)Penicillin (c2-6),alcoxi (C1-4)2. Alcox (C1-4) - tar (C1-4);Instead of phenyl, Alcoy (C1-6) or oy is a protective group of hydroxyl, halogen and hydrocarbon (C1-4),alquenilo (C2-6)Penicillin (c2-6),alcoxi (C1-4)Alcox (C1-4) - tar (C1-4),Trifluoroide; nitro, carboxy (C1-4),alcoxi (C1-4) -carbonilo carbonilo o ciano o bencilo con el resto fenilo del bencilo sustituido opcionalmente con alcoxi (C1-6) u OY en el que T es un grupo protector de hidroxi hal geno alquilo (C1-4)alquenilo (C2-6)Penicillin (c2-6),Alcox (C1-4) - tar (C1-4),3. Trifluoroamide, nitro, calcium carbonate (C1-4),Alcoy (C1-4) - carbide, carbide or cyanogen; AR is the halide AR of AR, which is composed of phenyl, naftil, pyridine, sulfur, furan, pyridyl alcohol, pyridyl, pyridyl glycol, pyridyl glycol, pyridyl glycol, oxazolilo, tiazolillo, pyridyl diene, pyrazolyl, pyrazolyl, pyridyl, pyridyl 1. One or more, preferably one or two, substitutes independently selected from halogen and tar (C1-4) groups can be selected to replace each monocrotophos;alquenilo (C2-6)Penicillin (c2-6),alcoxi (C1-4)Alcox (C1-4) - tar (C1-4),Sulfur trifluoride (CF3),1. Nitro, carboxy methoxy (C1-4),alcoxi (C1-4) -carbonilo carbonilos (cetonas y aldeh dos)Cyanogen; L is an activated group, such as halides, preferably iodized or brominated; or tar or hydrogen sulfide,Like messirato, three toed, coughing, with a double equation ligation (3),Among them: R6, R7, R8 and R9 are screened from hydrogen, cyclic or acyclic hydrocarbon (C1-6), alquenilo and arilo respectively; X and E are selected independently between hydrogen and oxygen; nitrogen is included in the form of ammonia or ammonia or as part of the isomerized nitrogen cycle; and oxygen is included in them. 1. In the presence of copper catalyst, a substitute of hydroxyl, oxygen or oxo is formed;