1043499-07-5

Upstream product

• 1043499-05-3 (R)-4-[(E)-2-(4-fluorophenyl)vinyl]-2,2-dimethyloxazolidine-3-carboxylic acid tert-butyl ester 
• 57009-75-3 2-(4-fluorophenyl)-1,3-dithiane 
• 1434253-88-9 C₂₁H₃₀FNO₃S₂ 
• 352-34-1 4-fluoro-1-iodobenzene 
• 115378-31-9 tert-butyl (4R)-2,2-dimethyl-4-vinyloxazolidine-3-carboxylate 
• 1434253-82-3 C₁₁H₂₀INO₃ 

Downstream Products

• 1043499-10-0 (R)-2-amino-4-(4-fluorophenyl)butan-1-ol 
• 1434254-20-2 tert-butyl N-[(2R)-4-(4-fluorophenyl)-1-hydroxybutan-2-yl]carbamate 
• 1217624-82-2 (2R)-2-{[(tert-butoxy)carbonyl]amino}-4-(4-fluorophenyl)butanoic acid 

Relevant academic research and scientific papers

FACTOR XIIA INHIBITORS

This invention relates to compoundsof formula (I)and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

Synthesis of γ-oxo γ-aryl and γ-aryl α-amino acids from aromatic aldehydes and serine

γ-Oxo α-amino acids and γ-aryl α-amino acids are compounds with very interesting biological properties and are active components of many drug molecules. Oxo amino acids are also used as synthetic precursors for a number of unnatural amino acids and amino alcohols. We report a very efficient synthesis of such compounds through the coupling of aromatic dithianes, prepared from aromatic aldehydes and an iodide derivative of serine. The dithiane groups in compounds thus obtained can be either hydrolyzed or reduced to generate 4-oxo-4-aryl or 4-aryl 2-amino butanol derivatives, respectively, which, on further transformations, can be converted into the title compounds. Starting with L-serine provides the corresponding D-amino acids with complete enantiopurity. The reported method is economically viable and complements the existing methods, which rely largely on cross-coupling reactions.

NOVEL 2-AMINOOXAZOLINES AS TAAR1 LIGANDS FOR CNS DISORDERS

The invention relates to the use of compounds of Formula (I) wherein R 1 is hydrogen, deuterium, tritium, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, phenyl optionally substituted by halogen, or is phenyloxy, benzyl, benzyloxy, -COO-lower alkyl, -O-(CH 2 ) o -O-lower alkyl, NH-cycloalkyl, cycloalkyl or tetrahydropyran-4-yloxy, wherein the substituents for n> 1 may be the same or different; X is a bond, -CHR-, -CHRCHR'-, -OCH 2 -, -CH 2 OCHR-, -CH 2 CH 2 CH 2 -, -SCH 2 -, -S(O) 2 CH 2 -, -CH 2 SCH 2 -, -CH 2 N(R)CH 2 -, -cycloalkyl-CH 2 - or SiRR'-CH 2 -; R/R' may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen, phenyl or lower alkyl; Y is phenyl, naphthyl, thiophenyl, pyridinyl, cycloalkyl, 1,2,3,4-tetrahydro-naphthalen-2-yl, 2,3-dihydrobenzo[1,4]dioxin-6-yl or benzo[1,3]dioxol-5-yl; n is 0, 1, 2 or 3; o is 2 or 3; or to a pharmaceutically suitable acid addition salt for the manufacture of medicaments for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders