- Preparation of differentiated diamides of 4,5,6,7-tetrahydropyrazolo[1,5-a] pyridine-2,6- and -3,6-dicarboxylic acids suitable for parallel synthesis
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1,3-Dipolar cycloaddition of a bicyclic sydnone to a propargylic acid amide affords 4,5,6,7-tetra-hydropyrazolo[1,5-a]pyridine-2,6- and -3,6-dicarboxylic acid monoamides which are further converted to corresponding differentiated diamides.
- Erdmane,Zemribo
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- Neuroleptic 2-substituted perhydro-1-h-pyrido[1,2-a]pyrazines
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Antipsychotic compounds having the formula STR1 wherein R is hydrogen, acyl or substituted acyl; and a pharmaceutically acceptable acid addition salt thereof.
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- Synthesis of trans-7-Hydroxymethyl-2-(2-benzisoxazol-3-yl)octahydro-2H-pyridopyrazine
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An efficient synthesis of trans-7-hydroxymethyl-2-(2-benzisoxazol-3-yl)octahydro-2H-pyridopyrazine 2 is presented which relies on the equilibration of cis-dimethyl piperidinedicarboxylate followed by alkylation with phthalimidoethyl triflate.
- Urban, Frank J.
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p. 857 - 862
(2007/10/02)
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- Process for preparing trans-piperidine-2,5-dicarboxylates
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Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a transsubstituted pyridine derivative of the formula STR1 wherein R is a (C1 -C3)alkyl group.
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- Neuroleptic perhydro-1H-pyrido[1,2-a]pyrazines
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Antipsychotic compounds having the formula STR1 wherein Z is H or Cl; Y is O or S; n is 1-4; separately, X is H or (C1 -C2)alkyl and L is R(CH2)m CO, m is 0 or 1-3, R is (C1 -C6)alkyl, (C3 -C7)cycloalkyl, phenyl, naphthyl, furyl, benzofuranyl, thienyl, benzothienyl, pyrrolyl, indolyl, isoindolyl or one of said groups substituted on aromatic or heteroaromatic ring with fluoro, chloro, (C1 -C2)alkyl or (C1 -C2)alkoxy; or together L and X, in combination with the nitrogen to which they are attached, form certain cyclic imides, 4-substituted piperidines or a cyclic sulfonamide.
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