摘要:
The invention is a highly efficient synthesis for making compounds of formula: ##STR1## wherein n=0, 1, R is C.sub.1-4 alkyl or benzyl; andR.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl or S--C.sub.1-4 alkyl. The process involves silane-mediated conjugation of 4-vinylpyridine to a substituted lactam.
摘要:
The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
摘要:
The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six membered saturated or unsaturated heterocyclic ring containing one or two heteroatoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
摘要:
An indole having the formula I: ##STR1## is prepared by a Fischer-Indole reaction employing a mixture of phosphorous pentoxide and methane sulfonic acid as an acid catalyst. The reaction, which is optionally run in a co-solvent, provides 3-unsubstituted indoles in high yields with high regioselectivity. The indole thus prepared is an intermediate in the synthesis of leukotriene biosynthesis inhibitors.
摘要:
Disclosed is an embossing system to be used with a die press. The embossing system includes a force transfer assembly, which comprises a first cover and an opposite second cover with the first and second covers being connected by a hinge. The force transfer assembly further includes a stencil and an opposing form positioned internal of the force transfer assembly. The stencil and the form are adapted to sandwich an embossing material, such as paper, between the stencil and the form. The embossing system further includes a layer of static vinyl that is located internally of one of the covers to secure the form to the internal side of one of the covers. The embossing system also utilizes an adhesive located on the cover opposite the cover with the vinyl to secure the stencil to the internal side of the opposite cover.
摘要:
A novel process for preparing 2-diazo-3-trisubstituted silyloxy-3-butenoates, synthons useful in the conversion of 3-substituted-4-acetoxy azetidinones and penicillin to thienamycin, imipenem and other carbapenem antibiotic compounds is provided, comprising the reaction of the appropriate diazo acetoacetate with the substituted silane, base and salt.
摘要:
An improved process is described which utilizes tetrachloro-1,4(or 1,2)-quinone as an oxidant in the Doebner-Miller synthesis of 7-chloroquinaldine, a starting material in the preparation of leukotriene antagonists. The process improves yield and eliminates the need of forming a ZnCl.sub.2 complex to isolate the end product.
摘要:
This invention relates to a process for preparing 2-(aminoalkylthio)carbapenems. In particular, this invention relates to a process in which a bis(substituted phenyl) phosphorohalidate is used to form an enol phosphate intermediate that can be converted to 2-(aminoalkylthio)carbapenems by reaction with suitable thioalkylamines.
摘要:
A process of synthesizing a compound of the formula 1: is disclosed, which comprises reacting a compound of the formula 2: with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
摘要:
A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.