Chemistry, design, and structure-activity relationship of cocaine antagonists.

@article{Singh2000ChemistryDA,
  title={Chemistry, design, and structure-activity relationship of cocaine antagonists.},
  author={S. Singh},
  journal={Chemical reviews},
  year={2000},
  volume={100 3},
  pages={
          925-1024
        }
}
  • S. Singh
  • Published 23 February 2000
  • Chemistry, Biology
  • Chemical reviews
H. Piperidine Analogues of Phenyltropanes 967 III. Cocaine Analogues 969 A. Stereoisomers of Cocaine 970 B. Phenyl Ring Substituted Cocaines 970 C. 2â-Substituted Cocaines 973 1. 2â-Substituted Cocaines 973 2. 2â-Substituted 4′-Iodococaines 977 D. N-Modified Cocaines 978 E. 3â-Carbamoyl Analogues of Cocaine 981 F. 3â-Alkylphenyltropanes 982 G. 6/7-Substituted Cocaine and Pseudococaine 982 H. 6-Alkyl-3-benzyltropanes 984 I. Piperidine Homologues of Cocaine 986 IV. 3R-Diphenylmethoxy Tropanes… 
Novel C-1 Substituted Cocaine Analogs Unlike Cocaine or Benztropine
TLDR
C-1 cocaine analogs with various C-1 substituents are not cocaine-like in that they are not stimulatory in vivo, however, they seem to interact with the DAT similarly to cocaine.
Enantioselective synthesis of cocaine C-1 analogues using sulfinimines (N-sulfinyl imines).
TLDR
The first examples of cocaine analogues having substituents at the C-1 position of the cocaine tropane skeleton were prepared by heating sulfinimine-derived α,β-unsaturated pyrrolidine nitrones to give tricyclic isoxazolidines that were transformed in three steps to the cocaine analogs.
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