Jeremiah P. Freeman
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View article: Reductive Methylation/Phosphorylation of 3,4-Diazacyclopentadienone N-Oxides with Trimethyl Phosphite
Reductive Methylation/Phosphorylation of 3,4-Diazacyclopentadienone N-Oxides with Trimethyl Phosphite Open
Treatment of 2,5-diphenyl-3,4-diazacyclopentadienone 3-oxide and 3,4-dioxide with trimethyl phosphite results in N-deoxygenation and methylation and O-phosphorylation to produce dimethyl (1-methyl-3,5diphenyl-4-pyrazolyl) phosphate.The rev…
View article: Extension of the SAR in the 1,2-Diaminocyclohexane Phenylacetamide Template
Extension of the SAR in the 1,2-Diaminocyclohexane Phenylacetamide Template Open
were prepared and allowed to extend the SAR of the U-50,488 template.
View article: Phenanthridone Analogs of the Opiate Agonist U-47,700 in the trans-1,2-Diaminocyclohexane Benzamide Series
Phenanthridone Analogs of the Opiate Agonist U-47,700 in the trans-1,2-Diaminocyclohexane Benzamide Series Open
View article: Syntheses of benzoquinolizidine and benzoindolizidine derivatives as anti-amnesic agents
Syntheses of benzoquinolizidine and benzoindolizidine derivatives as anti-amnesic agents Open
Tacrine, one of the drugs available for Alzheimer's disease based on the cholinergic approach, suffers from considerable toxicity. Many analogues of tacrine have been prepared which retain the pharmacologically rich aminopyridine or aminoq…
View article: Unusual C-C cleavage during reduction of a β-aminonitroalkene
Unusual C-C cleavage during reduction of a β-aminonitroalkene Open
An unusual ring cleavage product 3, a diamine, was observed during LAH reduction of β-aminonitroalkene1.
View article: Synthetic Studies towards A trans-3,4-Diamine Derivative of Piperidine Mimicking Buspirone
Synthetic Studies towards A trans-3,4-Diamine Derivative of Piperidine Mimicking Buspirone Open
& & .I & -Based on modeling experiment of buspirone we synthesized the sterically restricted analog, namely the piperidine 3,4-trans-amino amide (3).Preliminary biological evaluation is reported.The disclosure that buspirone (I), an anxiol…
View article: Anticonvulsants related to U-54494 prepared from cis-1,2- and cis-2,3-diaminotetralin
Anticonvulsants related to U-54494 prepared from cis-1,2- and cis-2,3-diaminotetralin Open
cis-Diaminotetralins 4 and 10 were converted in 4 steps to benzologs of the novel anticonvulsant U-54494. Attempted alkylation of 4 and 10 with 1,4-dibromobutane provided mixtures of the bis-pyrrolidino compounds and starting free bases to…
View article: Naphtho and benzo analogs of the .kappa. opioid agonist trans-(.+-.)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide
Naphtho and benzo analogs of the .kappa. opioid agonist trans-(.+-.)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide Open
Further elaboration on the structure-activity relationships in our U-50,488 series has revealed that benzologation of this cyclohexane-1,2-diamine derivative provides compounds which either maintain the interaction with the kappa receptor …
View article: The Synthesis of 9-(1-Azetidinyl)-1,2,3,4-tetrahydroacridine
The Synthesis of 9-(1-Azetidinyl)-1,2,3,4-tetrahydroacridine Open
tX&&&i -Synthesis of analogue (2) of tacrine is described in which the primary amino group is replaced by the azetidine moiety.The synthesis was accomplished in two steps from the acridinone derivative 10.This involved conversion of 1 0 to…
View article: Acid-catalyzed Cyclization of 2-Hydroxy-3-pyrrolone Derivatives. 2-Methoxy-3(2H)-furanones as Precursors of Polycyclic Nitrogen Heterocycles
Acid-catalyzed Cyclization of 2-Hydroxy-3-pyrrolone Derivatives. 2-Methoxy-3(2H)-furanones as Precursors of Polycyclic Nitrogen Heterocycles Open