摘要:
Methods of preparing compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
摘要:
The present invention concerns production of a compound of the formula or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: where Ar, Y, R1, Ry, R2, and m are as defined herein.
摘要:
Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
摘要:
Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
摘要:
Thiazolineazetidinone derivatives of the formulae 1,2, and 3. ##STR1## wherein R is derived from the commonly known carboxamido groups present in penicillins, R.sup.1 is a carboxy protecting group commonly used in penicillin chemistry, and R.sup.2 is Cl, Br, I, CN, lower alkoxy, lower acyloxy, SCN, SCH.sub.3, S-phenyl, S-heteroaryl such as 5-mercaptotetrazole or 2-mercapto-5-methyl-1,3,4-thiadiazole, NO.sub.3, N.sub.3, NH-phenyl, and N(CH.sub.3).sub.2 with the proviso that R.sup.2 in the compounds of formula 1 is limited to Cl, Br, I, and lower acyloxy, and a process for preparing said compounds from 2-(substituted methyl) penicillin sulfoxides followed by treatment with a base.The compounds of formulae 1,2, and 3 are useful as intermediates in the synthesis of cephalosporins.
摘要:
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.