摘要:
Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R8, A, A1 and n have the significance indicated in the specification.
摘要:
The present invention provides a process for the preparation of D-asparagine derivatives of formula I wherein R1 is an amino protecting group and R2 is an alkyl, a substituted alkyl or a group of formula A R3(OCH2CH2)n— A wherein R3 is hydrogen or an lower alkyl group and n is 1, 2 or 3, which process comprises reacting a compound of formula II wherein R1 and R2 are as defined above, with a protease in an aqueous solution at a pH of 6.0-7.5 and an organic solvent, and subsequently extracting the enantiomeric pure product of formula I. Compounds of formula I can be used as intermediates in the production of antibacterial substances.
摘要:
The present invention relates to a process for the preparation of a compound of formula I, wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen.(R)-2-phenyl propionic acid derivatives of formula I are key intermediates in the synthesis of 5-substituted-pyrazine or pyridine glucokinase activators of the formula Xa, which have the potential to be useful for the treatment and/or prophylaxis of type II diabetes.
摘要:
The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-γ-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-β-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.
摘要:
The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II wherein R21, R22, R23 and R24 are as defined in the description and claims.
摘要:
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.
摘要:
The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula starting from an isophthalic acid derivative of formula 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.
摘要:
The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-γ-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-β-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.
摘要:
The invention is concerned with new phosphine ligands of the formula I whereinR1 and R2 are independently of each other alkyl, aryl, cycloalkyl or heteroaryl, said alkyl, aryl, cycloalkyl or heteroaryl may be substituted by alkyl, alkoxy, halogen, hydroxy, amino, mono- or dialkylamino, aryl, —SO2—R7, —SO3−, —CO—NR8R8′, carboxy, alkoxycarbonyl, trialkylsilyl, diarylalkylsilyl, dialkylarylsilyl or triarylsilyl;R3 is alkyl, cycloalkyl, aryl or heteroaryl; R4′ and R4 signify independently of each other hydrogen, alkyl or optionally substituted aryl; or R4′ and R4 together with the C-atom they are attached to form a 3-8-membered carbocyclic ring; dotted line is absent or is present and forms a double bond; R5 and R6 are independently of each other hydrogen, alkyl or aryl; or linked together to form a 3-8-membered carbocyclic ring or an aromatic ring; R7 is alkyl, aryl or NR8R8′; and R8 and R8′ are independently of each other hydrogen, alkyl or aryl;metal complexes with such ligands as well as the use of such metal complexes as catalysts in asymmetric reactions.
摘要:
The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.