77663-31-1

Upstream product

• 1504-06-9 3-methylindolin-2-one 

Downstream Products

• 88239-76-3 6-Methyl-5-oxo-1-(toluene-4-sulfonyl)-1,2,3,4,5,6-hexahydro-benzo[b]azocine-4-carboxylic acid methyl ester 
• 88239-71-8 4-[[2-(1-Methoxycarbonyl-ethyl)-phenyl]-(toluene-4-sulfonyl)-amino]-butyric acid ethyl ester 
• 88239-77-4 6-Methyl-5-oxo-1-(toluene-4-sulfonyl)-1,2,3,4,5,6-hexahydro-benzo[b]azocine-4-carboxylic acid ethyl ester 
• 88239-72-9 2-{2-[(3-Cyano-propyl)-(toluene-4-sulfonyl)-amino]-phenyl}-propionic acid methyl ester 
• 88239-78-5 6-Methyl-5-oxo-1-(toluene-4-sulfonyl)-1,2,3,4,5,6-hexahydro-benzo[b]azocine-4-carbonitrile 
• 36797-38-3 methyl 2-(2-p-toluenesulfonylamidophenyl)propionate 
• 344872-37-3 2-[2-(Toluene-4-sulfonylamino)-phenyl]-propionic acid 

Relevant academic research and scientific papers

Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl group, and the pharmaceutical compositions in which they are present

This invention relates to compounds of formula STR1 in which: R1 and R2 are similar or different and are each independently hydrogen or a group selected from CO2 N=C(NH2)2, CONHNHCONH2, CONHNHCSNH2, C(OC2 H5)=NCO2 CH3, COCH2 CO2 H5, N(OH)-CONHCOOC2 NCO2 CH3, COCH2 CO2 H5, N(OH)-CONHCOOC2 H5, C(OC2 H5)=NH or a nitrogen heterocycle; with the proviso that at least one of the substituents R1 or R2 is other than hydrogen; R3 is a hydrogen, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C3 -C7 cycloalkyl, a phenyl, a phenylalkyl, or a phenylalkenyl; R4 and R5 are each independently a C1 -C6 alkyl, a C3 -C7 cycloalkyl, a phenyl or a phenylalkyl; or R4 and R5, bonded together, are either a group of the formula (CH2)n or a group of the formula (CH2)p Y (CH2)q, in which Y is either an oxygen atom, or a sulfur atom, or a substituted carbon atom, or a group N-R6, in which R6 is a hydrogen, a C1 -C4 alkyl, a phenylalkyl, a C1 -C4 alkylcarbonyl, a C1 -C4 halogenoalkylcarbonyl, a C1 -C4 polyhalogenoalkylcarbonyl, a benzolyl, an α-aminoacyl or a N-protecting group, or R4 and R5, together with the carbon atom to which they are bonded, form an indane or an adamantine; p+q=m; n is an integer between 2 and 11; m is an integer between 2 and 5; X is an oxygen or a sulfur atom; and z and t are zero or z+t=1; and its salts.

SYNTHESIS OF 1,2,3,4-TETRAHYDRO-1-BENZAZOCIN-5(6H)-ONES BY DIECKMANN CONDENSATION

Tetrahydro-1-benzazocin-5(6H)-ones (5,6,8-10) have been conveniently prepared by the Dieckmann condensation of the diester 1 and 3, or the ester nitrile 4 by using sodium-potassium alloy as an effective base.