Abstract: Provided is a process for preparing 4-borono-L-phenylalanine, which has steps of: reacting N-protected (S)-4-halophenylalanine of formula (I), a boronating agent and an organolithium to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of formula (II) and the R group represents a protecting group; isolating the N-protected (S)-4-boronophenylalanine from the reaction mixture; deprotecting the R group of the N-protected (S)-4-boronophenylalanine to obtain L-BPA.

Abstract: Provided is a process for preparing 4-borono-L-phenylalanine, which has steps of: reacting N-protected (S)-4-halophenylalanine of formula (I), a boronating agent and an organolithium to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of formula (II) and the R group represents a protecting group; isolating the N-protected (S)-4-boronophenylalanine from the reaction mixture; deprotecting the R group of the N-protected (S)-4-boronophenylalanine to obtain L-BPA.

Abstract: Provided is a compound of the following formula (I) for preparing 4-(10B)borono-L-phenylalnine: wherein R group represents a protecting group and is selected from the group consisting of: tert-butoxycarbonyl (Boc) group, trityl (Trt) group, 3,5-dimethoxyphenylisopropoxycarbonyl(Ddz) group, 2-(4-Biphenyl)isopropoxycarbonyl (Bpoc) group, and 2-nitrophenylsulfenyl (Nps) group, and the compound has a 10B purity higher than or equal to 98% and an enantiomeric excess higher than or equal to 99%.

Abstract: 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.

Abstract: Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.

Abstract: 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.

Abstract: This invention is directed to methods of preparing compounds of formula (I): comprising the step of reacting a compound of formula (II): with a reagent of formula POX3 and silica gel at a temperature greater than about 75° C., and wherein substitutions at X, PG, A, G, R1 and R4 are set forth in the specification.

Abstract: The invention provides a process for recovering CCI-779 from mother liquors.

Abstract: 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.

Abstract: A method for regioselective synthesis of CCl-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method.

Abstract: The invention provides a process for recovering CCI-779 from mother liquors.

Abstract: Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: A method and apparatus for continuously processing fiber into an elastomeric component uses an expanding die (11, 11a) for orienting fibers in other than the processing direction of the extrusion. In one embodiment, an injection mold (50) is used with the expanding die (11), and in another embodiment, an extruder (30) is used with expanding die (11a). Processing parameters may be alteredto control the direction of orientation of fibers (20) in the elastomer component. Orientation of fibers (20) in an extrudate (17) is dependent on the processing speed viscosity of the elastomer, pressure of extrusion, the length l1 and l2 and height h1 and h2 of gate (12) and expansion cavity (14), respectively, of the expansion die (11, 11a).

Abstract: A method for regioselective synthesis of CCl-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method.

Abstract: This invention provides a regioselective process for preparing a 42-ester or ether of rapamycin, and 31-silyl ether intermediates.

Abstract: This invention provides a regioselective process for preparing a 42-ester or ether of rapamycin, and 31-silyl ether intermediates.

Abstract: A method for molding short fiber/rubber composite articles having enhanced mechanical properties by aligning short reinforcing fibers during an injection molding process. The method comprises injecting a molding mixture through an injection gate arranged in a predetermined relationship to the molding cavity. The injection gate has a relatively small thickness in comparison to the thickness of the molding cavity. The fibers are associated with a first direction, generally parallel to the flow of the molding mixture as the molding mixture moves through the gate. As the molding mixture passes through the gate and into the cavity, the fiber direction is altered as the molding material fills the cavity.