77232-48-5

Upstream product

• 22536-61-4 2-chloro-5-methylpyrimidine 
• 960-16-7 tributylphenylstannane 
• 1670-14-0 benzamidine monohydrochloride 
• 42588-57-8 3-ethoxymethacrolein 
• 68906-00-3 2-phenyl-5-nitropyrimidine 
• 6407-34-7 methyl-1 ethylideneamine 
• 74222-83-6 benzamidine hydrochloride hydrate 
• 920518-65-6 3-dimethyl-amino-2-methylpropenal 
• 98-80-6 phenylboronic acid 
• 108805-57-8 N,N,N',N'-tetramethyl-2-methyl-malondialdehyde diimine hydrochloride 
• 100-47-0 benzonitrile 
• 95804-09-4 N-Triphenylphosphoranyliden-benzamidin 
• 104322-41-0 (+)-(2R)-benzyloxy-2,5-dihydrofuran-4-carboxaldehyde 

Downstream Products

• 122773-97-1 2-phenylpyrimidine-5-carboxylic acid 
• 77232-36-1 2-(p-Brommethyl-phenyl)-5-methyl-pyrimidin 
• 77232-11-2 <4-(5'-Methylpyrimidin-2'-yl)phenylmethyl>phosphonsaeure-diaethylester 
• 1637587-29-1 2-(5-methylpyrimidin-2-yl)benzonitrile 
• 122773-96-0 2-phenylpyrimidine-5-carboxylic acid amide 
• 122774-00-9 2-phenylpyrimidine-5-carbonyl chloride 
• 85386-15-8 2-phenylpyrimidine-5-carbonitrile 
• 85386-14-7 2-phenylpyrimidine-5-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Ruthenium-Catalyzed meta-Selective C?H Mono- and Difluoromethylation of Arenes through ortho-Metalation Strategy

The first example for the ruthenium-catalyzed ligand-directed meta-selective C?H mono- and difluoromethylation is developed, affording a variety of new meta-mono- and difluoromethylated 2-phenylpyridines, 2-phenylpyrimidines, and 1-phenylpyrazoles in moderate-to-good yields. This new transformation exhibits broad substrate scope, good functional group tolerance, and high efficiency, and offers a practical approach to synthesize mono- and difluoromethylated arenes. Mechanistic studies indicate that a reaction pathway involving palladium-initiated radical species is involved in the catalytic cycle. The new dual catalytic system consisting of compatible ruthenium(II) and palladium(0) complexes enables the key processes of C?H activation and mono-/difluoromethyl-radical formation to occur and achieves the meta-selective functionalization efficiently. In addition, the present protocol can also be extended to non-fluoromethylation.

A arylpyrimidines and its derivatives preparation method (by machine translation)

This invention has offered a kind of arylpyrimidines and process for preparing derivatives thereof, comprising the following steps: S1) shown in the formula (II) 2 the iminium salts dial two substituted propionic [...], shown in formula (III) compound with a nitrile group of alkaline catalyst 1st reaction in the organic solvent, get mixed solution; S2) in the mixed solution is added with ammonium salt and 2nd alkaline catalyst, for the reaction, formula (I) shown in the arylpyrimidines and its derivatives. Compared with the prior art, this invention is in the presence of the alkaline catalyst, 2 the iminium salts dial two substituted propionic [...], of nitrile compounds and ammonium salt [3+2 + 1] ternary cyclization reaction to construct a pyrimidine ring, in order to get arylpyrimidines and its derivatives, this method does not use the noble metal catalyst, line is simple, low cost, high controllability of the process, easy industrialization, reduces the waste of relatively high yield and emissions. (by machine translation)

Copper-catalyzed, oxidative sp2 C-H cyanation: Facile synthesis of aromatic carbonitriles

Cu(OAc)2-catalyzed regioselective oxidative C-H cyanation of two different types of aromatics was described, providing facile access to functionalized heterocycles in good yields. Control experiments suggest the copper chelation-assisted oxidative C-H activation mechanism. ARKAT-USA, Inc.

SELECTIVE CYP11B1 INHIBITORS FOR THE TREATMENT OF CORTISOL DEPENDENT DISEASES

The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.

N-AROYLAMINO ACID AMIDES AS ENDOTHELIN INHIBITORS

The present invention relates to the compounds of formula (I) STR1 wherein R is carboxy, esterified carboxy, carbamoyl, N-(alkyl or aryl)-carbamoyl, cyano, 5-tetrazolyl or CONH--SO 2--R 4 ; R. sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R 2 is hydrogen or lower alkyl, or R 1 and R 2 represent lower alkylene to form together with the carbon and nitrogen atoms to which they are attached an azacycloalkane ring; R 3 is heterocyclic or carbocyclic (aryl or biaryl)-lower alkyl; Y is lower alkylidenyl, 3-to 10-membered cycloalkylidenyl which may be substituted by oxo, alkylenedioxy, hydroxy, acyloxy, lower alkoxy; or Y is 5-to 10-membered cycloalkylidenyl fused to a saturated or unsaturated carbocyclic 5-or 6-membered ring; or Y is 5-to 8-membered oxacycloalkylidenyl, 5-to 8-membered (thia-, oxothia-or dioxothia-) cycloalkylidenyl, or 5-to 8-membered azacycloalkylidenyl optionally N-substituted by lower alkyl or aryl-lower alkyl; R 4 represents hydrogen, lower alkyl, carbocyclic aryl, heterocyclic aryl, cycloalkyl, (carbocyclic aryl, heterocyclic aryl, cycloalkyl, hydroxy, acyloxy, or lower alkoxy)-lower alkyl, lower alkyl substituted by carboxyl, by esterified carboxyl or by amidated carboxyl; Ar represents carbocyclic or heterocyclic aryl; and pharmaceutically acceptable salts thereof; which are useful as endothelin inhibitors in mammals.

Iminophosphoranes in heterocyclic chemistry. A simple one-pot synthesis of dihydropyrimidines and pyrimidines

The condensation of N-triphenylphosphoraniliden-benzamidine with acyclic α,β-unsaturated aldehydes produces dihydropyrimidines in good to high yields. The methodology has been extended to alicyclic and heterocyclic aldehydes.

Regiochemistry in Pd-Catalysed Organotin Reactions with Halopyrimidines

Chlorines in activated pyrimidine position is replaced by carbon substituents in Pd-catalysed reactions with organotin compounds.The 4(6)-position is more reactive than the 2-position allowing for regioselective coupling in 2,4(6)-dihalopyrimidines.A bromine substituent is required for coupling in the benzenoid 5-position.In 5-bromo-2,4-dichloropyrimidine the 4-chlorine is replaced before the 5-bromine and the latter before the 2-chloro substituent, all in a regioselective manner.The methodology can be used to introduce functionalized carbon substituents into any pyrimidine position.

Ueber die Herstellung von Styryl- und Stylbenyl-Derivaten des Pyrimidins

2- and 4-(p-Tolyl)-substituted pyrimidines react with anils of hetero-aromatic aldehydes in the presence of dimethylformamide and potassium hydroxide or potassium t-butoxide to yield the corresponding 2- and 4-pyrimidines or