704910-29-2

Upstream product

• 928150-63-4 N,N-diethyl(α,α-difluoro-4-methoxybenzyl)amine 
• 3373-59-9 L-threonine methyl ester 
• 7465-86-3 4-methoxy-N,N-diethylbenzamide 
• 100-07-2 4-methoxy-benzoyl chloride 
• 704910-28-1 (2S,3R)-3-hydroxy-2-(4-methoxybenzamido)-butyric acid methyl ester 

Downstream Products

• 704910-30-5 methyl (4S,5R)-4-{[(benzyloxy)methyl]}-4,5-dihydro-2-(4-methoxyphenyl)-5-methyloxazole-4-carboxylate 
• 860453-75-4 (4R,5R)-4-((S)-1-Hydroxy-2-methyl-propyl)-2-(4-methoxy-phenyl)-5-methyl-4,5-dihydro-oxazole-4-carboxylic acid methyl ester 
• 860453-67-4 (4S,5R)-4-[(S)-1-(tert-Butyl-dimethyl-silanyloxy)-2-methyl-propyl]-2-(4-methoxy-phenyl)-5-methyl-4,5-dihydro-oxazole-4-carboxylic acid methyl ester 
• 860453-68-5 (2R,3S)-2-Acetyl-3-(tert-butyl-dimethyl-silanyloxy)-2-(4-methoxy-benzylamino)-4-methyl-pentanoic acid methyl ester 
• 857311-65-0 (2R,3S)-2-Acetyl-2-[acryloyl-(4-methoxy-benzyl)-amino]-3-(tert-butyl-dimethyl-silanyloxy)-4-methyl-pentanoic acid methyl ester 
• 860453-69-6 (2R,3S)-2-[(S)-1-(tert-Butyl-dimethyl-silanyloxy)-2-methyl-propyl]-3-hydroxy-1-(4-methoxy-benzyl)-3-methyl-4-methylene-5-oxo-pyrrolidine-2-carboxylic acid methyl ester 
• 860453-76-5 (2R,3S,4R)-2-[(S)-1-(tert-Butyl-dimethyl-silanyloxy)-2-methyl-propyl]-3-hydroxy-4-(2-hydroxy-ethyl)-1-(4-methoxy-benzyl)-3-methyl-5-oxo-pyrrolidine-2-carboxylic acid methyl ester 
• 860453-71-0 (3R,3aS,7aR)-3-[(S)-1-(tert-Butyl-dimethyl-silanyloxy)-2-methyl-propyl]-2-(4-methoxy-benzyl)-3a,5,5-trimethyl-1-oxo-octahydro-4-oxa-2-aza-5-sila-indene-3-carboxylic acid methyl ester 
• 860453-70-9 (2R,3S)-2-[(S)-1-(tert-Butyl-dimethyl-silanyloxy)-2-methyl-propyl]-3-(iodomethyl-dimethyl-silanyloxy)-1-(4-methoxy-benzyl)-3-methyl-4-methylene-5-oxo-pyrrolidine-2-carboxylic acid methyl ester 
• 704910-34-9 methyl (2R,3S)-1-(4-methoxybenzyl)-2-((benzyloxy)methyl)-3-hydroxy-3-methyl-4-methylene-5-oxopyrrolidine-2-carboxaldehyde 
• 704910-35-0 methyl (2R,3R)-1-(4-methoxybenzyl)-2-((benzyloxy)methyl)-3-hydroxy-3-methyl-4-methylene-5-oxopyrrolidine-2-carboxaldehyde 
• 704910-43-0 (2R,3R)-2-Benzyloxymethyl-2-(4-methoxy-benzylamino)-3-trimethylsilanyloxy-butyric acid methyl ester 
• 704910-33-8 methyl (R)-2-(N-(4-methoxybenzyl)acrylamido)-2-((benzyloxy)methyl)-3-oxybutanoate 
• 704910-32-7 methyl (2R,3R)-2-(N-(4-methoxybenzyl)acrylamido)-2-((benzyloxy)methyl)-3-hydroxybutanoate 

Relevant academic research and scientific papers

METHOD FOR PRODUCING 2-OXAZOLINE ANALOGUE OR 1,3-OXAZINE ANALOGUE

The present invention is a method for producing a 2-oxazoline analogue or a 1,3-oxazine analogue represented by the following general formula (3) by reacting a 1,2-aminoalcohol compound or a 1,2-aminothiol compound with an α,α-dihaloamine compound. (In the formula, n represents 0 or 1, and R represents an oxygen atom or a sulfur atom. R1, R2 and R3 each represents an atom or a group shown in Group 1 to Group 3, and R° represents an atom or a group shown in Group 2 or Group 3. Two or more of R1, R2 and R3 may be bonded to each other to form a ring. Group 1: a hydrogen atom, a halogen atom, a nitro group, a cyano group, a formyl group, a carboxyl group, a sulfonyl group, a sulfinoyl group or a sulfenyl group; Group 2: an alkyl group, which may have an arbitrary substituent, an aryl group or an aralkyl group; and Group 3: an alkyl-substituted, aryl-substituted or aralkyl-substituted oxy group, a carbonyl group, an oxycarbonyl group, a carbonyloxy group, a thio group, a sulfonyl group, a sulfinoyl group or a sulfenyl group)

A facile synthesis of oxazolines, thiazolines, and imidazolines using α,α-difluoroalkylamines

β-Amino alcohols, β-amino thiols, and β-diamines can be converted to the corresponding oxazoline, thiazoline, and imidazoline derivatives, respectively, by reaction with α,α-difluoroalkylamines under mild conditions. The reaction is applicable for the synthesis of optically active heterocyclic compounds. Georg Thieme Verlag Stuttgart.

ANALOGS OF SALINOSPORAMIDE A

Disclosed herein are analogs of Salinosporamide A, having the Formulae Ia - IVa as follows: [insert chemical formula here] Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.

Simple stereocontrolled synthesis of salinosporamide A

A simple and effective stereocontrolled synthesis of salinosporamide A (1) has been developed which follows the pathway outlined in the Figure. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).

A simple stereocontrolled synthesis of salinosporamide A

A simple and effective stereocontrolled synthesis of salinosporamide A has been developed. This process, the first synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. Salinosporamide A was of special interest as a synthetic target because of its potent in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less). Copyright