C07D263/12

SOLID-SUPPORTED PALLADIUM (II) COMPLEX AS A HETEROGENEOUS CATALYST FOR CROSS COUPLING REACTIONS AND METHODS THEREOF

A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions.

Azoline ring-containing compound, electron transport/injection layer material containing the same, and organic electroluminescent element using the same

An object is to provide an azoline ring-containing compound which achieves characteristics required for an organic EL element, such as a driving voltage, a quantum efficiency, and element lifetime in a well-balanced manner, and particularly can obtain a high quantum efficiency, for example, in a case where the azoline ring-containing compound is used for the organic EL element. The above object is achieved by an azoline ring-containing compound represented by the following general formula (1). ##STR00001## In formula (1), φ represents an m-valent group derived from an aromatic hydrocarbon having 6 to 40 carbon atoms or the like, Y represents —O—, —S—, or >N—Ar, R.sup.1 to R.sup.5 each represent a hydrogen atom or an alkyl having 1 to 4 carbon atoms, and L represents a phenylene group or the like.

Azoline ring-containing compound, electron transport/injection layer material containing the same, and organic electroluminescent element using the same

An object is to provide an azoline ring-containing compound which achieves characteristics required for an organic EL element, such as a driving voltage, a quantum efficiency, and element lifetime in a well-balanced manner, and particularly can obtain a high quantum efficiency, for example, in a case where the azoline ring-containing compound is used for the organic EL element. The above object is achieved by an azoline ring-containing compound represented by the following general formula (1). ##STR00001## In formula (1), φ represents an m-valent group derived from an aromatic hydrocarbon having 6 to 40 carbon atoms or the like, Y represents —O—, —S—, or >N—Ar, R.sup.1 to R.sup.5 each represent a hydrogen atom or an alkyl having 1 to 4 carbon atoms, and L represents a phenylene group or the like.

COMPOUND OF 3,3,3',3'-TETRAMETHYL-1,1'-SPIROBIINDANE-BASED BISOXAZOLINE LIGAND, INTERMEDIATE THEREOF, PREPARATION METHOD THEREOF AND USE THEREOF
20210363135 · 2021-11-25 ·

Provided are a compound of 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based bisoxazoline ligand, an intermediate, a preparation method and uses thereof. The compound of bisoxazoline ligand is a compound having a structure represented by formula I, or an enantiomer, a raceme, or diastereomer thereof. The bisoxazoline ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6′-dihydroxyl-3,3,3′,3′-tetramethyl-1,1′-spirobiindane is used as a starting raw material and the compound represented by formula II serves as the key intermediate through a series of reactions. The new bisoxazoline ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral bisoxazoline ligand that is widely used in many asymmetric catalytic reactions of metal catalysis, and thus it has economic practicability and industrial application prospect.

##STR00001##

Compound of 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based bisoxazoline ligand, intermediate thereof, preparation method thereof and use thereof
11220495 · 2022-01-11 · ·

Provided are a compound of 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based bisoxazoline ligand, an intermediate, a preparation method and uses thereof. The compound of bisoxazoline ligand is a compound having a structure represented by formula I, or an enantiomer, a raceme, or diastereomer thereof. The bisoxazoline ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6′-dihydroxyl-3,3,3′,3′-tetramethyl-1,1′-spirobiindane is used as a starting raw material and the compound represented by formula II serves as the key intermediate through a series of reactions. The new bisoxazoline ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral bisoxazoline ligand that is widely used in many asymmetric catalytic reactions of metal catalysis, and thus it has economic practicability and industrial application prospect. ##STR00001##

SYNTHESIS OF HETEROCYCLIC COMPOUNDS FROM CARBOXAMIDE AND CARBOXAMIDE DERIVATIVES WITH HALOALKANOLS

The invention provides for methods for the synthesis of various compounds through reaction of carboxamide, or carboxamide derivatives, with various substituted or unsubstituted haloalkanols in a one-step, single vessel, reaction mechanism. Preferably, but not exclusively, the reaction proceeds in the absence of any solvents, catalyst, base, or any further reagents.

SYNTHESIS OF HETEROCYCLIC COMPOUNDS FROM CARBOXAMIDE AND CARBOXAMIDE DERIVATIVES WITH HALOALKANOLS

The invention provides for methods for the synthesis of various compounds through reaction of carboxamide, or carboxamide derivatives, with various substituted or unsubstituted haloalkanols in a one-step, single vessel, reaction mechanism. Preferably, but not exclusively, the reaction proceeds in the absence of any solvents, catalyst, base, or any further reagents.

Max binders as MYC modulators and uses thereof

The present disclosure provides compounds of Formula (I), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits. ##STR00001##

Manganese (III) catalyzed C—H aminations

Reactions that directly install nitrogen into CH bonds of complex molecules are significant because of their potential to change the chemical and biological properties of a given compound. Selective intramolecular CH amination reactions that achieve high levels of reactivity, while maintaining excellent site-selectivity and functional-group tolerance is a challenging problem. Herein is reported a manganese perchlorophthalocyanine catalyst [Mn.sup.III(ClPc)] for intermolecular benzylic CH amination of bioactive molecules and natural products that proceeds with unprecedented levels of reactivity and site-selectivity. In the presence of Brnsted or Lewis acid, the [Mn.sup.III(ClPc)]-catalyzed CH amination demonstrates unique tolerance for tertiary amine, pyridine and benzimidazole functionalities. Mechanistic studies indicate that CH amination proceeds through an electrophilic metallonitrene intermediate via a stepwise pathway where CH cleavage is the rate-determining step of the reaction. Collectively these mechanistic features contrast previous base-metal catalyzed CH aminations. The catalyst can be a compound of Formula I: ##STR00001##

Manganese (III) catalyzed C—H aminations

Reactions that directly install nitrogen into CH bonds of complex molecules are significant because of their potential to change the chemical and biological properties of a given compound. Selective intramolecular CH amination reactions that achieve high levels of reactivity, while maintaining excellent site-selectivity and functional-group tolerance is a challenging problem. Herein is reported a manganese perchlorophthalocyanine catalyst [Mn.sup.III(ClPc)] for intermolecular benzylic CH amination of bioactive molecules and natural products that proceeds with unprecedented levels of reactivity and site-selectivity. In the presence of Brnsted or Lewis acid, the [Mn.sup.III(ClPc)]-catalyzed CH amination demonstrates unique tolerance for tertiary amine, pyridine and benzimidazole functionalities. Mechanistic studies indicate that CH amination proceeds through an electrophilic metallonitrene intermediate via a stepwise pathway where CH cleavage is the rate-determining step of the reaction. Collectively these mechanistic features contrast previous base-metal catalyzed CH aminations. The catalyst can be a compound of Formula I: ##STR00001##