摘要:
[PROBLEMS] To provide a process for efficient production of optically active β-hydroxy-α-aminocarboxylic acid derivatives of anti conformation useful as intermediates of drugs or agricultural chemicals. [MEANS FOR SOLVING PROBLEMS] A process for the production of optically active β-hydroxy-α-aminocarboxylic acid derivatives represented by the general formula (2) or (3): [wherein R1 is substituted or unsubstituted C1-20 alkyl or a substituted or unsubstituted C4-12 aromatic group; and R2 is substituted or unsubstituted C1-20 alkyl or a substituted or unsubstituted C4-12 aromatic group], characterized by hydrogenating an α-aminoacylacetate ester represented by the general formula (1): [wherein R1 and R2 are each as defined above] through catalytic asymmetric hydrogenation in the presence of an acid.
摘要:
The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and derivatives thereof. The alpha-amino acids and derivatives thereof may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate, and a C1-C6 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.
摘要:
The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
摘要:
The present invention relates to new processes for the preparation of gabapentin by the desilylation of a silylated gabapentin or by the silylation-desilylation of an acid addition salt of gabapentin with a silylating agent.
摘要:
The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
摘要:
When a basic amino acid is produced by culturing a microorganism having an ability to produce the basic amino acid in a liquid medium under an aerobic condition to produce and accumulate the basic amino acid in the medium, pH of the medium is controlled to be 6.5-9.0 during the culture, and 7.2-9.0 at the end of the culture, and a culture period where 2 g/L or more of hydrogencarbonate ions and/or carbonate ions exist in the medium is secured during the culture by controlling pressure in a fermentation tank to be a positive pressure during the fermentation, or supplying carbon dioxide gas or a mixed gas containing carbon dioxide gas to the medium, so that the hydrogencarbonate ions and/or carbonate ions should serve as counter ions of cations mainly consisting of the basic amino acid.
摘要:
The invention relates to a new process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid of formula (I) via the new intermedier 1-(nitromethyl)cyclohexyl-acetic acid derivative of formula (II), wherein R represents hydrogen, benzyl group, diphenylmethyl group or C1-C4 alkyl or alkoxy aromatic ring substituted derivatives thereof.
摘要:
Compounds of formula (I) wherein: R1, R2 which are the same or different, are a hydrogen atom, or a -(CH2)m-O-(CH2)n-R3 group, wherein R3 is an aryl residue, m is an integer 1 to 5 and n is an integer 1 to 4, with the proviso that R1 and R2 cannot be at the same time hydrogen, as well as the optically active forms of the chelates thereof with Mn(II) and the salts thereof with physiologically compatible organic bases selected from primary, secondary, tertiary amines or basic amino acids, or with inorganic bases whose cations are sodium, potassium, magnesium, calcium, or mixtures thereof, are disclosed.