15159-67-8

Upstream product

• 15159-66-7 α-amino-γ-bromobutyric acid methyl ester hydrochloride 
• 501-53-1 benzyl chloroformate 
• 5672-83-3 Z-L-GluOMe 
• 104523-50-4 N-hydroxypyridine-2-selenone 
• 4668-42-2 (S)-2-benzyloxycarbonylamino-succinic acid 1-methyl ester 
• 67-56-1 methanol 
• 15159-65-6 (2S)-2-amino-4-bromobutanoic acid hydrobromide 
• 4668-37-5 N-(benzyloxycarbonyl)asparagine methyl ester 
• 2304-96-3 N-benzyloxycarbonyl-L-asparagine 
• 23632-67-9 (S)-3-[3-(benzyloxycarbonyl)-5-oxooxazolidin-4-yl]propanoic acid 
• 314728-04-6 (S)-2-benzyloxycarbonylamino-4-hydroxybutyric acid methyl ester 
• 2185-03-7 L-homoserine lactone hydrochloride 
• 58578-43-1 (S)-2-benzyloxycarbonylamino-4-hydroxybutyric acid dicyclohexylamine salt 
• 35677-88-4 N-benzyloxycarbonyl-(L)-homoserine 

Downstream Products

• 15159-68-9 N^α'-Benzyloxycarbonyl-L-cystathionin-α'-methylester; (L-2-Amino-7-benzyloxycarbonylamino-4-thiaoctan-1-saeure-8-saeuremethylester 
• 104523-60-6 (2S)-2-benzyloxycarbonylamino-4-phenylselenyl-butyric acid methyl ester 
• 84677-05-4 methyl 1-(((benzyloxy)carbonyl)amino)cyclopropane-1-carboxylate 
• 30134-53-3 S-4-Cyano-2-[[(phenylmethoxy)carbonyl]-amino]butanoic acid methyl ester 
• 255737-46-3 (2S), 2-(benzyloxycarbonylamino), 4-[(3S), 3-benzyloxycarbonylamino, 3-methoxycarbonyl propyldisulfanyl]-butyric acid methyl ester 
• 864682-69-9 (S)-2-benzyloxycarbonylamino-4-hydroxyphosphinoyl-butyric acid methyl ester 
• 1026613-99-9 C₂₀H₃₂NO₆PSi 
• 875668-29-4 (S)-2-[(3-benzyloxycarbonylamino-3-methoxycarbonyl-propyl)-methoxy-phosphinoylmethyl]-pentanedioic acid 

Relevant academic research and scientific papers

A Simple Synthesis of 1-Aminocyclopropane-1-carboxylic Acid

Conversion of N-carbobenzyloxy-L-glutamic acid α-methylester (Z-L-glu(OH)OCH3, 1) into the bromo derivative 2 and subsequent γ-elimination by the use of sodium hydride leads to the fully protected synthon 3 in good yields.Deprotection by sodium hydroxide and hydrogenolysis yields almost quantitively the key substance 5.

HERBICIDAL COMPOSITIONS

The present invention relates herbicidal combinations and their use in controlling plants or inhibiting plant growth. In particular, herbicidal combinations of the invention comprise at least one pyridazine derivative of Formula (I) as defined herein, in combination with at least one further herbicide that is a pyrrolidinone derivatives of the Formula (II) as defined herein.

HERBICIDAL COMPOSITIONS

The present invention relates novel herbicidal combinations and their use in controlling plants or inhibiting plant growth. In particular, herbicidal combinations of the invention comprise at least one pyridazine derivative as defined herein, in combination with at least one futher herbicide that is an acetoclactase synthase (ALS) inhibitor.

HERBICIDAL COMPOSITIONS

The present invention relates to novel herbicidal combinations and their use in controlling plants or inhibiting plant growth. In particular, herbicidal combinations of the invention comprise at least one pyridazine derivative of Formula (I), in combination with at least one futher herbicide that is a non-selective herbicide, a herbicide that acts through the inhibition of protoporphoryinogen oxidase, or a herbicide that inhibits photosystem II in photosynthesis.

HERBICIDAL COMPOSITIONS

The present invention relates to herbicidal combinations and their use in controlling plants or inhibiting plant growth. In particular, herbicidal combinations comprising at least one pyridazine derivative of Formula (I) as defined herein, in combination with at least one further herbicide that is a compound of Formula (II) as defined herein.

PRE-HARVEST DESICCATION METHOD

A method for the pre-harvest desiccation of crop plants which comprises applying to the crop plants an effective amount of a compound of formula (I) or an agronomically acceptable salt or zwitterionic species thereof, wherein the substituents are as defined in claim 1.

HERBICIDAL COMPOSITIONS

The present invention relates novel herbicidal combinations and their use in controlling plants or inhibiting plant growth. In particular, herbicidal combinations of the invention comprise at least one pyridazine derivative of Formula (I), in combination with at least one futher herbicide that is a HPPD-inhibitor herbicide, a synthetic AUXIN herbicide, a herbicide that acts through the inhibition of ACCase, or a herbicide that inhibits cell division through interference with VLCFA biosynthesis.

HERBICIDAL COMPOUNDS

Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.

4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic Acid Butyl Ester (ACT-246475) and Its Prodrug (ACT-281959), a Novel P2Y12 Receptor Antagonist with a Wider Therapeutic Window in the Rat Than Clopidogrel

Recent post hoc analyses of several clinical trials with P2Y12 antagonists showed the need for new molecules being fully efficacious as antiplatelet agents and having a reduced propensity to cause major bleeding. We have previously reported the discovery of the 2-phenylpyrimidine-4-carboxamide analogs as P2Y12 antagonists with nanomolar potency in the disease-relevant platelet aggregation assay in human plasma. Herein we present the optimization steps that led to the discovery of clinical candidate ACT-246475 (30d). The key step was the replacement of the carboxylic acid functionality by a phosphonic acid group which delivered the most potent molecules of the program. In addition, low in vivo clearance in rat and dog was achieved for the first time. Since the bioavailability of 30d was low in rat and dog, we developed the bis((isopropoxycarbonyl)oxy)methyl ester prodrug (ACT-281959, 45). Compound 30d showed efficacy in the rat ferric chloride thrombosis model when administered intravenously as parent or orally as its prodrug 45. Moreover, 30d displays a wider therapeutic window as compared to clopidogrel in the rat surgical blood loss model.

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.