2 step process for preparing biologically active tropane derivat

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...


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Preparation of biologically active tropane derivatives of novel configurations. The compounds are prepared by decomposing vinyldiazomethanes in the presence of pyrroles to provide a bicyclic ring containing the basic tropane ring system which is then reacted with an aryl Grignard reagent in the presence of a copper (I) or (II) salt to provide 3-aryl-tropane derivatives.

patent: 3120537 (1964-02-01), Archer et al.
patent: 3813404 (1974-05-01), Clarke et al.
Boja, et al., "New Potent Cocaine Analogs: Ligand Binding and Transport Studies in Rat Striatum", European Journal of Pharmacology, 184 (1990) 329-332.
Carroll, et al., "Synthesis, Ligand Binding, QSAR and CoMFA Study of 3.beta.-Carbixylic Acid Methyl Esters", Journal of Medicinal Chemistry, vol. 34, No. 9 (1991), p. 2719-2725.
Clarke, et al., "Compounds Affecting the Central Nervous System.4. 3.beta.-Phenyltropane-2-Carboxylic Esters and Analogs", Journal of Medicinal Chemistry, vol. 16, No. 11 (1973) pp. 1260-1267.
"Synthesis of (.+-.)-Ferruginine and (.+-.)-Anhydroecgonine Methyl Ester By a Tandem Cyclopropanation/Cope Rearrangement", J.Org.Chem., vol. 56, No. 19 (1991) p. 5696-5700.
Madras, et al. "Cocaine Receptors Labeled by [.sup.3 H]2.beta.-(4-Fluorophenyl Tropane", Molecular Pharmacology, 36:;518-524 (1989).
Davies, et al., "Novel Entry to the Tropane System by Reaction of Rhodium (II) Acetate Stabilized Vinylcarbenoids with Pyrroles", Tetrahedron Letters, vol. 30, No. 35, pp. 4653-4656 (1989).
Davies et al., "Chemistry of Vinylcarbenoids with a Single Electron Withdrawing Group. An Approach to Tropane Alkaloids" American Chemical Society, Dec. 5-7, 1990, pp. 181-182.


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