369611-56-3

Upstream product

• 1159502-39-2 (R)-2-benzyloxycarbonylamino-4-hydroxybutyric acid, dicyclohexylamine salt 
• 74-88-4 methyl iodide 
• 41088-85-1 N-[(phenylmethoxy)carbonyl]-D-homoserine 
• 501-53-1 benzyl chloroformate 
• 1152-62-1 (2R)-2-[[(benzyloxy)carbonyl]amino]-4-(methylsulfanyl)butanoic acid 
• 41088-89-5 D-2-<(benzyloxycarbonyl)amino>-4-butyrolactone 

Downstream Products

• 82179-05-3 (R)-2-benzyloxycarbonylamino-4-bromo-butyric acid methyl ester 
• 1159502-43-8 4-[(R)-2-benzyloxycarbonylamino-4-(diethoxy-phosphoryl)-butyryl]-piperazine-1-carboxylic acid ethyl ester 
• 1159502-40-5 (R)-2-benzyloxycarbonylamino-4-(diethoxy-phosphoryl)-butyric acid methyl ester 
• 1159502-41-6 (R)-2-benzyloxycarbonylamino-4-(diethoxy-phosphoryl)-butyric acid 
• 637008-57-2 R-2-benzyloxycarbonylamino-4-phthalimidooxybutyric acid methyl ester 

Relevant academic research and scientific papers

NOVEL CLOSTRIDIUM DIFFICILE TOXIN INHIBITORS

The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.

SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES

The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES

The present invention relates to compounds of formula (I) wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

PHOSPHONIC ACID DERIVATES AND THEIR USE AS P2Y12 RECEPTOR ANTAGONISTS

The invention relates to 2-phenyl-pyrimidine derivatives containing a phosphonic acid motif and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. (I).

Cyclic hydroxamates, especially multiply substituted [1,2]oxazinan-3-ones

Routes to putative N-acyl-D-ala-D-ala surrogates, beginning with the conversion of 4-, 5-, and 6-membered lactones into 5-, 6-, and 7-membered cyclic hydroxamates, are reported. The key step of the synthesis is trimethylaluminium-promoted cyclization of an ω-aminooxyester. The 7-membered cyclic hydroxamate crystallizes in a chair conformation. Extension of the reaction sequence to homoserine or homoserine lactone leads to cyclocanaline and N-acylated cyclocanalines. The 4-phenylacetamido derivative of cyclocanaline crystallizes in a boat conformation. The attachment of a 2-carboxypropyl substituent to the ring nitrogen of a 4-acylaminocyclocanaline has been effected, prior to cyclization, by coupling of the acyclic aminooxyester precursor to the triflate of benzyl lactate or, after cyclization, by coupling to tert-butyl α-bromopropionate in the presence of potassium fluoride - alumina, followed by removal of the protecting group in each case. A six-membered homolog of the antibiotic lactivicin has been synthesized by the reaction of 4-phenylacetamidocyclocanaline with benzyl 2-oxoglutarate in the presence of carbodiimide, followed by hydrogenolysis. Starting with methyl 2,4-dibromo-2,4-dideoxy-L-erythronate, which is available in two steps from L-ascorbic acid, these reaction sequences have been applied to the stereospecific synthesis of a D-alanine derivative whose nitrogen atom is enclosed within a 3,4-disubstituted [1,2]oxazinan-3-one.