522654-02-0Relevant articles and documents
The Barbier - Grignard-type carbonyl alkylation using unactivated alkyl halides in water
Keh, Charlene C. K.,Wei, Chunmei,Li, Chao-Jun
, p. 4062 - 4063 (2003)
The aqueous Barbier-Grignard-type alkylation of aldehydes with unactivated alkyl iodides and bromides was developed. By using a combination of zinc and cuprous iodide, catalyzed by indium(I) chloride, we successfully added tertiary, secondary, and primary alkyl halides to various aromatic aldehydes in 0.07 M aqueous Na2C2O4. A mechanistic rationale for the success of the reaction has been proposed. Copyright
A Phosphine-Free Manganese Catalyst Enables Stereoselective Synthesis of (1 + n)-Membered Cycloalkanes from Methyl Ketones and 1, n-Diols
Adhikari, Debashis,Das, Kuhali,Jana, Akash,Kundu, Abhishek,Maji, Biplab,Thorve, Pradip Ramdas
, p. 2615 - 2626 (2020/03/11)
Herein, we report the stereoselective synthesis of (1 + n)-membered cycloalkane from methyl ketone and 1,n-diol. A manganese(I) complex bearing a phosphine-free ligand catalyzed the reaction, which involved the formation of two C-C bonds via a sequence of
Structure-activity relationship of trihexyphenidyl analogs with respect to the dopamine transporter in the on going search for a cocaine inhibitor
Dar,Thiruvazhi,Abraham,Kitayama,Kopajtic,Gamliel,Slusher,Carroll,Uhl
, p. 1013 - 1021 (2007/10/03)
A series of trihexyphenidyl (THP) analogs were used to search for a derivative that could serve as a cocaine inhibitor. A compound that blocks binding of the cocaine analog carboxyfluorotropane (CFT), allows dopamine uptake and exhibits low side effects could serve as a good candidate for that purpose. All analogs were tested for the extent to which they inhibit CFT binding, dopamine uptake and n-methyl scopolamine (NMS) binding. Several structure-function relationships emerged. Methylation/halogenation of THP's benzene ring enhanced the compound's ability to block CFT binding in comparison to its ability to block dopamine uptake (5a-e). Replacement of the cyclohexyl ring with a benzene ring tended to create compounds that had lower affinities to the dopamine transporter (7b compared to THP, 7d compared to 5h, 7c compared to 8c) and modification of THP's piperidine ring tended to enhance affinity to the dopamine transporter (5f-h, 8a, 8c). One analog (5f) that showed little muscarinic activity indicating that it would probably have few side effects was investigated for its effects as an in vivo cocaine inhibitor. However, it showed few antagonistic effects in vivo. Nevertheless, this work greatly elucidates the structure-function relationships required for potential cocaine inhibitors and so lays out promising directions for future research.
