Chiral N-substituted allylic amine compounds

    公开(公告)号:US12129268B2

    公开(公告)日:2024-10-29

    申请号:US17239991

    申请日:2021-04-26

    摘要: The method relates to the field of asymmetric allylic amination and comprises preparing a chiral N-substituted allylic amine compound from the corresponding allylic substrates and substituted hydroxylamines, in the presence of a catalyst, said catalyst comprising copper compounds and a chiral ligand. Examples of chiral amine compounds which can be made using the method include Vigabatrin, Ezetimibe Terbinafine, Naftifine 3-methylmorphine, Sertraline, Cinacalcet, Mefloquine hydrochloride, and Rivastigmine. There are over 20,000 known bioactive molecules with chiral N-substituted allylic amine substructure. The method may also be used to produce non-natural chiral ß-aminoacid esters, a sub-class of chiral N-substituted allylic amine compounds. Examples of ß-aminoacid ester which can be produced by the disclosed method, include, but are not limited to, N-(2-methylpent-1-en-3-yl)benzenamine and Ethyl 2-methylene-3-(phenylamino)butanoate. Further, the products of the method described herein can be used to produce chiral heterocycles and bioactive molecules or materials. A novel chiral copper-BINAM nitrosoarene complex is also set forth.

    Anti-cancer composition containing gold and cytotoxic agent

    公开(公告)号:US12110301B2

    公开(公告)日:2024-10-08

    申请号:US18606890

    申请日:2024-03-15

    IPC分类号: A61P35/00 C07F1/00

    CPC分类号: C07F1/005 A61P35/00

    摘要: A gold(III) complex of formula (I) or formula (II)






    wherein R1 and R2 are each independently a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted arylalkyl, or an optionally substituted aryl; R3 and R4 are each independently a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted arylalkyl, an optionally substituted aryl, an optionally substituted heterocyclyl, an optionally substituted alkoxy, a hydroxyl, a halo, a nitro, a cyano, a N-monosubstituted amino group, or a N,N-disubstituted amino group; and X is Cl, Br, or I. A pharmaceutical composition containing the gold(III) complex of formula (I) or (II), and a method of treating cancer are included.

    Liquid pharmaceutical composition of gold

    公开(公告)号:US12110300B2

    公开(公告)日:2024-10-08

    申请号:US18606361

    申请日:2024-03-15

    IPC分类号: A61P35/00 C07F1/00

    CPC分类号: C07F1/005 A61P35/00

    摘要: A gold (III) complex of formula (I) or formula (II)






    wherein R1 and R2 are each independently a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted arylalkyl, or an optionally substituted aryl; R3 and R4 are each independently a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted arylalkyl, an optionally substituted aryl, an optionally substituted heterocyclyl, an optionally substituted alkoxy, a hydroxyl, a halo, a nitro, a cyano, a N-monosubstituted amino group, or a N,N-disubstituted amino group; and X is Cl, Br, or I. A pharmaceutical composition containing the gold(III) complex of formula (I) or (II), and a method of treating cancer are included.

    Synthesis of tetrazolate salts
    8.
    发明授权

    公开(公告)号:US11773112B2

    公开(公告)日:2023-10-03

    申请号:US17542235

    申请日:2021-12-03

    IPC分类号: C07F1/00 C07F1/08 C07D257/06

    CPC分类号: C07F1/08 C07D257/06

    摘要: The present invention relates to a novel method of synthesis of copper (I) 5-nitrotetrazolate. Particularly, for the synthesis of the copper (I) 5-nitrotetrazolate, the present invention uses a suitable salt of 5-aminotetrazole, preferably the sulfate or the nitrate salt as the starting compound. The selection of the said starting chemical not only eliminates any safety issue arising during Sandmeyer reaction conditions to affect the functional group conversion but also greatly improves the ease of executing the synthetic protocol, rendering the process safe to be adopted for commercial manufacture of the copper (I) 5-nitrotetrazolate compound.