1484-93-1

Upstream product

• 61809-48-1 3-methoxy-N-(phenylaminocarbonyl)2-methyl-2-propenamide 
• 66003-76-7 Diphenyliodonium triflate 
• 65-71-4 2,4-dihydroxy-5-methylpyrimidine 
• 108-86-1 bromobenzene 
• 65-71-4 thymin 
• 98-80-6 phenylboronic acid 
• 1193318-81-8 1-(3-ethoxy-2-methylacryloyl)-3-phenylurea 
• 62-53-3 aniline 
• 4330-20-5 N-3-benzoylthymine 

Relevant academic research and scientific papers

Phenylation of pyrimidinones using diphenyliodonium salts

Pyrimidinones 1 have been phenylated under basic conditions using diphenyliodonium salts, and the effect of substituents on the yield and regiochemistry has been studied. The Royal Society of Chemistry 1999.

COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS

Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

A convenient, high-yield synthesis of 1-substituted uracil and thymine derivatives

Novel reagents for the synthesis of 1-substituted uracil and thymine derivatives have been developed. The aminolysis of 2- or 4-nitrophenyl 3-ethoxyacryloylcarbamate and 3-ethoxy-2-methylacryloylcarbamate with a variety of primary amino derivatives procee

A mild and efficient method for N-arylnucleobase synthesis via the cross-coupling reactions of nucleobases with arylboronic acids catalyzed by simple copper salts

A simple and efficient copper-salt catalyzed N-arylation of nucleobases is reported. In a mixed solvent of MeOH and H2O, the coupling products were obtained in moderate to excellent yields at room temperature within a short time. Avariety of su

Efficient N-arylation and N-alkenylation of the five DNA/RNA nucleobases

(Chemical Equation Presented) A general approach to N-arylation and N-alkenylation of all five DNA/RNA nucleobases at the nitrogen atom normally attached to the sugar moiety in DNA or RNA has been developed. Various protected or masked nucleobases engaged

Hypervalent iodine in synthesis: Part 86. Selective copper-catalyzed N-monoarylation and N1,N3-diarylation of uracil and its derivatives with diaiyliodonium salts

N-Arylation of uracil and its derivatives 2 with diaryliodonium salts 1 was investigated in order to explore a new synthetic methodology associated with N-aryluracil derivatives. In the presence of K2CO3, the copper-catalyzed arylation gave N1,N3-diarylation products with high selectivity and in good yields (Table 2). However, the use of NaOAc as the base in the copper-catalyzed arylation of 6-methyluracil (2a) resulted in N3-arylation products with high selectivity, and, in the copper-catalyzed arylation of uracil (2b) or 5-methyluracil (=thymine; 2c), N1-arylation products were the major products (Table 3).

PYRIMIDINEDIONE, PYRIMIDINETRIONE, TRIAZINEDIONE AND TETRAHYDROQUINAZOLINEDIONE DERIVATIVES AS ALPHA1-ADRENERGIC RECEPTOR ANTAGONISTS

Compounds of Formula I: STR1 where R 5 is a group selected from Formulae (a), (b), (c) and (d): STR2 and the pharmaceutically acceptable salts and N-oxides thereof, are α 1-adrenergic receptor antagonists useful for the treatment of diseases involving directly or indirectly an obstruction of the lower urinary tract, such as benign prostatic hyperplasia.

Pyrimidinedione, pyrimidinetrione, triazinedione, tetrahydroquinazolinedione derivatives as alpha-1-adrenergic receptor antagonists

The present invention relates to novel α1-adrenoceptor antagonists of the formula I*(formula 01)* in which: R1 is acetylamino, amino, cyano, trifluoroacetylamino, halo, hydro, hydroxy, nitro, methylsulfonylamino, 2-propynyloxy, a group selected from (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-4)alkyl, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C3-6)cycloalkyl(C1-4)alkyloxy and (C1-4)alkylthio (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl, aryloxy, aryl(C1-4)alkyloxy, heteroaryloxy and heteroaryl(C1-4)alkyloxy (which aryl and heteroaryl are optionally further substituted with one to two radicals independently selected from halo and cyano); R2 is cyano, halo, hydro, hydroxy or a group selected from (C1-6)alkyl and (C1-6)alkyloxy (which group is optionally further substituted with one to three halogen atoms);R3 and R4 are both hydro or methyl or together are ethylene; and R5 is a group selected from Formulae (a), (b), (c) and (d):*(formula 02)* in which: X is C(O), CH2 or CH(OH); Y is CH2 or CH(OH); Z is N or C(R9), wherein R9 is hydro, (C1-6)alkyl or hydroxy; R6 is hydro, a group selected from (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-4)alkyl (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, heteroaryl, aryl(C1-4)alkyl and heteroaryl(C1-4)alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C1-6)alkyloxy, (C1-6)alkyl and aryl); R7 is (C1-6)alkanoyl, carbamoyl, cyano, di(C1-6)alkylamino, halo, hydro, hydroxy, hydroxyiminomethyl, (C1-6)alkylsulfonyl, (C1-6)alkylthio, a group selected from (C1-6)alkyl, (C3-6)cycloalkyl,(C1-6)alkyloxy and (C1-6)alkyloxy(C1-4)alkyl (which group is optionally further substituted with one to three radicals selected from halo, hydroxy or (C1-6)alkyloxy) or a group selected from aryl, heteroaryl, aryl(C1-4)alkyl and heteroaryl(C1-4)alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C1-6)alkyloxy, (C1-6)alkyl and aryl) or R7 and R9 together are tetramethylene; and each R8 is independently hydro, hydroxy, methyl or ethyl; and the pharmaceutically acceptable salts and N-oxides thereof.