Pharmaceutical Compositions and Methods for Effecting Dopamine Release
a technology of dopamine and composition, applied in the field of pharmaceutical compositions, can solve the problems of profound decline in the psychosocial affect of the subject suffering therefrom, difficulty in concentrating, listening, learning and completing tasks, restlessness, fidgety, etc., and achieve the effects of reducing the number of nicotinic cholinergic receptors of the brain of the patient, preventing and suppressing symptoms, and modulating neurotransmitter secretion
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example 1
[0110] Sample No. 1 is (+ / −)-2-(3-pyridyl)-1-azabicyclo[2.2.2]octane, which is prepared in accordance with the techniques set forth in U.S. Pat. No. 5,559,124, the disclosure of which is incorporated herein by reference in its entirety.
example 2
[0111] Sample No. 2 is (+ / −)-2-(5-bromo-3-pyridyl)-1-azabicyclo[2.2.2]octane, which is prepared in accordance with the following techniques. The techniques employed in the synthesis of the oxanyl-4-methanol are described by Thomas and Clough, J. Pharm. Pharmacology, 15: 167 (1963).
Diethyl oxane-4,4-dicarboxylate
[0112] Sodium (20.7 g, 900 mmol) was carefully dissolved in dry ethanol (300 mL) and to this mixture was added diethyl malonate (144 g, 900 mmol) and 2, bis-(2-chloroethyl)ether (129 g, 900 mmol). The reaction mixture was refluxed for 15 h and cooled to room temperature. The solvent was removed by rotary evaporation, the product acidified with 10% HCl (200 mL), extracted with ethyl acetate (4×200 mL) and dried (Na2SO4). Removal of solvent by rotary evaporation, followed by distillation (170-175° C., 22 mm Hg) furnished the product (98.0 g, 48% yield).
Oxane-4,4-dicarboxylic acid
[0113] To a stirred solution of diethyl oxane-4,4-dicarboxylate (40.0 g., 173 mmol) in ethanol (...
example 3
[0129] Sample No. 3 is exo 2-(3-pyridyl)-1-azabicyclo[2.2.1]heptane, which is prepared according to the following techniques.
N-(Diphenylmethylidene)-3-(aminomethyl)pyridine
[0130] Benzophenone (10.92 g, 60 mmol), 3-(aminomethyl)pyridine (6.48 g, 60 mmol) and p-toluenesulfonic acid (10 mg) were dissolved in 30 mL benzene and the reaction mixture was heated to reflux under a nitrogen atmosphere using a Dean-Stark apparatus. The completion of the reaction (12-16 h) was determined when the calculated amount of water was collected in the Dean-Stark apparatus. Benzene was removed by rotary evaporation and the resulting N-(diphenylmethylidene)-3-(aminomethyl)pyridine was used in the next step without further purification.
3-Oxolanylmethyl methanesulfonate
[0131] Methanesulfonyl chloride (18 mmol, 1.39 mL) was added to a flask containing oxolanyl-3-methanol (1.53 g, 15.0 mmol) in THF (25 mL) and triethylamine (3.13 mL, 22.5 mmol) at 0° C. under a nitrogen atmosphere. The cooling bath was r...
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Abstract
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