30134-53-3

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 2650-67-1 (R)-2-Benzyloxycarbonylamino-4-carbamoyl-butyric acid methyl ester 
• 773837-37-9 sodium cyanide 
• 314728-04-6 (S)-2-benzyloxycarbonylamino-4-hydroxybutyric acid methyl ester 
• 127105-49-1 methyl (2S)-2-amino-4-(tetrazol-5-yl)-butyrate 
• 15159-67-8 (2S)-2-benzyloxycarbonylamino-4-bromo-butyric acid methyl ester 
• 143-33-9 sodium cyanide 
• 151-50-8 potassium cyanide 
• 13907-82-9 N²-benzyloxycarbonyl-L-glutamine methyl ester 

Downstream Products

• 15231-21-7 (S)-2-((phenylmethoxycarbonyl)amino)-4-cyanobutanoic acid 
• 65882-90-8 methyl (2S)-2-(benzyloxycarbonylamino)-4-(tetrazol-5-yl)butyrate 
• 30134-54-4 (S)-2-Benzyloxycarbonylamino-4-cyano-butyric acid 2,4,5-trichloro-phenyl ester 
• 30134-55-5 ((S)-2-Benzyloxycarbonylamino-4-cyano-butyrylamino)-acetic acid ethyl ester 
• 165754-55-2 HUN-7293 

Relevant academic research and scientific papers

Bis-morpholinophosphorylchloride, a novel reagent for the conversion of primary amides into nitriles

Bis-morpholinophosphorylchloride (Bmpc), in the presence of a base, is an efficient dehydrating agent for both aromatic and aliphatic primary amides, and gives corresponding nitriles under mild conditions in god yields and purity. During the reaction the enantiomeric integrity remains intact.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Carbapenem biosynthesis: Confirmation of stereochemical assignments and the role of CarC in the ring stereoinversion process from L-Proline

(5R)-Carbapen-2-em-3-carboxylic acid is the simplest structurally among the naturally occurring carbapenem β-lactam antibiotics. It co-occurs with two saturated (3S,5S)- and (3S,5R)-carbapenam carboxylic acids. Confusion persists in the literature about t

Quinazoline thymidylate synthase inhibitors

The invention relates to quinazoline derivatives or pharceutically-acceptable salts thereof, which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 is (1-4C)alkyl; the quinazoline ring may optionally bear one or two further substituents selected from halogeno, (1-4C)alkyl and (1-4C)alkoxy; R2 is hydrogen or (1-4C)alkyl; R3 includes hydrogen and (1-4C)alkyl; and Ar is optionally substituted phenylene or heterocyclene; or a pharmaceutically-acceptable salt or ester thereof.

Total synthesis of HUN-7293

The first total synthesis of the cyclic heptadepsipeptide HUN-7293 (1), a potent inhibitor of cell adhesion molecule expression exhibiting anti-inflammatory properties, is detailed. The most effective approach relied on an unusually efficient macrocyclization with the formation of the MLEU3 - LEU4 secondary amide that potentially benefits from intramolecular H-bonding preorganization of the acyclic substrate. The requisite linear depsipeptide was convergently assembled with the late stage introduction of the linking ester enlisting a Mitsunobu esterification that occurs with inversion of the DGCN α-center permitting the utilization of a readily available L-amino acid precursor to the D α-hydroxy carboxylic acid residue. An alternative and similarly attractive approach of direct macrolactonization of a substrate necessarily incorporating a D-DGCN subunit proved viable albeit less effective. Biological evaluation in cellular assays for vascular adhesion molecule expression confirmed that synthetic HUN-7923 (1) is essentially indistinguishable from the naturally occurring cyclodepsipeptide.

Tricyclic compounds with pharmaceutical activity

The invention relates to tricyclic compounds of formula (I) STR1 wherein R1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R3 includes a group of the formula --NHCH(CO2 H)--A1 --Y1 wherein A1 is (1-6C)alkylene and Y1 is carboxy, tetrazol-5-yl, N-?(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.

Non-glutamate type pyrrolo[2,3-d]pyrimidine antifolates. I: Synthesis and biological properties of pyrrolo[2,3-d]pyrimidine antifolates containing tetrazole congener of glutamic acid

Either the α- or γ-carboxyl group of the glutamic acid moiety of N-[4-[3-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)propyl] benzoyl]-L-glutamic acid (1b, TNP-351) and its related compound (1a) was replaced with a 1H-tetrazole ring, and the in

Process for preparing nitriles

A facile and mild process for the preparation of nitriles from reagent sensitive primary carboxamides is described. The process utilizes a (carboxysulfamoyl)ammonium hydroxide compound as the dehydrating agent. It is useful for preparing nitriles which ha

AN EFFICIENT CHEMOSELECTIVE SYNTHESIS OF NITRILES FROM PRIMARY AMIDES

An efficient chemoselective method for the preparation of nitriles from primary amides is described which utilizes methyl (carboxysulfamoyl)triethylammonium hydroxide inner salt (Burgess reagent) as the dehydrating reagent.