86096-97-1

Upstream product

• 18424-77-6 sodium diethyl methylmalonate 
• 86096-88-0 m-nitrobenzyl mesitoate 
• 609-08-5 Diethyl methylmalonate 
• 619-23-8 3-Nitrobenzyl chloride 
• 619-25-0 3-Nitrobenzyl alcohol 

Downstream Products

• 138711-97-4 (S)-(+)-2-(3-nitrobenzyl)propionic acid 
• 138711-93-0 methyl 3-aminophenyl-2-methylpropionate 
• 66735-02-2 (+/-)-2-methyl-3-(3-nitro-phenyl)-propionic acid 
• 66735-02-2 (R)-2-(3-nitrobenzyl)propionic acid 
• 29417-82-1 2-methyl-3-(3-nitrophenyl)-propionic acid methyl ester 

Relevant academic research and scientific papers

Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the b2 adrenergic receptor

The present invention provides a compound of formula (I): wherein: R1 is a group selected from -CH2OH,-NHCOH and R2 is a hydrogen atom; or R1 together with R2 form the group -NHC(O)CH=CH-, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2, R3a and R3b are independently selected from the group consisting of hydrogen atoms and C1-4 alkyl groups n is an integer selected from 0 to 6, R4 is selected from the group consisting of an optionally substituted monocyclic or polycyclic C3-10 cycloalkyl group, an optionally substituted monocyclic C5-10 aryl group and, a methyl group which is substituted with one or more substituents selected from C5-10 aryl and C5-10 aryloxy groups, wherein the monocyclic or polycyclic C3-10 cycloalkyl and the monocyclic C5-10 aryl groups independently are optionally substituted with one or more substituents selected from halogen atoms, C1-4 alkyl, C1-4 alkoxy, C5-10 aryl and C5-10 aryloxy groups, or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.

Integrin expression inhibitors

The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR4bR5b)mb— (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

INTEGRIN EXPRESSION INHIBITORS

The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, -CH=CH- or - (CR4bR5b)mb- (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or -CO-NH-; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

CHEMOENZYMATIC SYNTHESIS OF THE ENANTIOMERS OF IOPANOIC ACID

The two enantiomers of Iopanoic acid 1 were prepared in enantiomeric excess higher than 90percent by enzyme-catalyzed hydrolysis of precursors (+/-)-2a and (+/-)-3a, followed by standard chemical transformations.Among the tested enzymes, chymotrypsin and Lipase PS proved to be the most selective catalysts.The stereochemical outcome of the lipase-catalyzed hydrolyses of esters (+/-)-2a-d is strictly dependent upon both the size of the alkyl group attached to the chiral center and the substituent in the aromatic ring.The enantioselectivity of the reactions was evaluated by chiral HPLC and the configurations of the new products were assigned by chemical correlations.

Nucleophilic Substitution Reactions in m-Nitrobenzylic Substrates

The reaction of m-nitrobenzyl 2,4,6-trimethylbenzoate (11) with the salt (2) of 2-nitropropane, or the thiolate (16), gives moderate yields of substitution products .However, the mechanism of formation of these products could not be defi