Patent classifications
B01J2531/824
Method of preparing metal complexes of formula Z-M, in particular carbene-metal complexes
The present invention relates to an improved method of preparing metal complexes, in particular carbene-metal complexes. The method comprises the step of subjecting a salt of formula Z.sup.+—X.sup.− and a non-ionic metal salt of formula ML.sub.n or subjecting a metallate of formula Z.sup.+ . . . ML.sub.nX.sup.− to a mechanical mixing process in the presence of a base. The method allows to formation of heterocyclic carbene metal complexes such as a nitrogen-containing heterocyclic carbene (NHC)-metal complexes. The invention also relates to the use of metal complexes, in particular carbene-metal complexes such as heterocyclic carbene-metal complexes obtainable by the method according to the present invention as catalysts.
Process for producing aromatic compound, and palladium complex
A process for producing an aromatic compound in high yield and a palladium complex are provided. The palladium complex is represented by formula (D) or formula (D′): ##STR00001##
In formula (D), X represents a chlorine atom, A represents an alkyl group having 1 to 3 carbon atoms, B represents an alkyl group having 4 to 20 carbon atoms or a cycloalkyl group having 5 to 10 carbon atoms, R.sup.4 and R.sup.5 each independently represent a hydrogen atom, a fluorine atom, or an alkoxy group having 1 to 20 carbon atoms, and R.sup.6, R.sup.7 and R.sup.8 represent a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms or a heteroaryl group having 4 to 20 carbon atoms. ##STR00002##
In formula (D′), X, A, B and R.sup.4 to R.sup.8 are the same as defined above.
PARP/PI3K DOUBLE-TARGET INHIBITOR CONTAINING PYRIDOPYRIMIDINE STRUCTURE
The present disclosure relates to the field of pharmaceutical chemistry, in particular to a class of PARP/PI3K double-target inhibitors (I) containing structures of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine and phthalazin-1(2H)-one and a preparation method thereof. As proved by pharmacodynamic tests, the compounds of the present disclosure have PARP/PI3K double-target inhibitory activity and can be used for anti-tumor.
Synthesis of Cannabigerol
Multiple methods of synthesizing cannabigerol are presented. Combining olivetol with geraniol derivatives are provided. Cross-coupling methods of combing functionalized resorcinols are provided. Useful intermediates are formed during such cross-coupling steps.
ALKOXYCARBONYLATION OF TRIVINYLCYCLOHEXANE
Process for the alkoxycarbonylation of trivinylcyclohexane.
REDUCTION METHOD AND REDUCTION PRODUCT OF ALKENYL ACTIVE METHYLENE COMPOUND
Disclosed are a reduction method and reduction product of an alkenyl active methylene compound. The reduction reaction comprises the following steps: taking an alkenyl active methylene compound as a substrate, a metal hydride as a reducing agent, and a palladium compound as a catalyst, performing a reduction reaction to obtain a reduction product, and then reducing the alkenyl active methylene compound. The reduction system is a simple method for reducing the alkenyl active methylene compound, and the used hydride and palladium compound catalyst are both reagents that could easily be obtained in a laboratory. Compared with conventional hydrogen hydrogenation methods and reduction methods of reducing agents, the method is easier to operate, higher in safety, mild in conditions, and high in reaction yield, a reaction in a one-pot two-step manner can be achieved, and high atom economy and step economy can be obtained.
Synthesis of cannabigerol
Multiple methods of synthesizing cannabigerol are presented. Combining olivetol with geraniol derivatives are provided. Cross-coupling methods of combing functionalized resorcinols are provided. Useful intermediates are formed during such cross-coupling steps.
METHOD FOR SYNTHESIZING INDOMETHACIN AND ANALOGUE THEREOF
The present disclosure belongs to the technical field of indomethacin synthesis, and discloses a method for synthesizing an indomethacin and an analogue thereof. The method for synthesizing an indomethacin and an analogue thereof includes steps of: introducing an alkyl group, an aromatic ring or a heteroaromatic ring directly at the C2 position of indole, a carboxylic acid fragment at the C3 position of the indole, and an aroyl group at the N1 position of the indole through palladium-catalyzed reactions. The present disclosure solves a problem: most of the existing indomethacin synthesis methods are achieved by construction of an indole ring and modification; simple structural changes of an indomethacin molecule based on this synthetic strategy often require de novo synthesis; the late modification and structure-activity relationship study of the indomethacin molecule have lengthy synthetic steps.
Palladium acyclic diaminocarbene complexes as precatalysts for Hiyama coupling and the tandem one-pot fluoride free Hiyama coupling/cyclization for the synthesis of biologically relevant
The present invention provides Acyclic diaminocarbene complex of formula (I): ##STR00001##
Wherein, M is palladium; X is monoanionic ligand selected from Cl, Br or I; Where R1 is different from R2; R1 is selected from the group consisting of alkyl or aryl, each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms; R2 is selected from the group consisting of alkyl, or aryl each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms. The said palladium diamino carbine complex of the present invention are particularly useful as catalyst from Hiyama cross-coupling reaction.
TRI-(ADAMANTYL)PHOSPHINES AND APPLICATIONS THEREOF
In one aspect, phosphine compounds comprising three adamantyl moieties (PAd.sub.3) and associated synthetic routes are described herein. Each adamantyl moiety may be the same or different. For example, each adamantyl moiety (Ad) attached to the phosphorus atom can be independently selected from the group consisting of adamantane, diamantane, triamantane and derivatives thereof. Transition metal complexes comprising PAd.sub.3 ligands are also provided for catalytic synthesis including catalytic cross-coupling reactions.