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    • 4. 发明授权
    • Preparation of 1-aminoalkylamino-9-orothioxanthene-4-carbox-aldehydes
    • 1-氨基甲酰氨基-9-异二氢-4-羧酸 - 醛酸的制备
    • US3764612A
    • 1973-10-09
    • US3764612D
    • 1970-10-05
    • STERLING DRUG INC
    • COLLINS JROSI D
    • C07D335/16A61K27/00C07D65/18
    • C07D335/16
    • 1-(R1R2N-Y-NH)-9-oxothioxanthene-4-carboxaldehydes, intermediates for the preparation of the corresponding 4hydroxymethyl compounds, are prepared by heating 1-chlorothioxanthen-9-one with R1R2N-Y-NHCH3 to yield 1-(R1R2N-Y-NH(CH3)) thioxanthen-9-one, reacting the latter compound with phosphorus oxyhalide and dimethylformamide to yield 1-(R1R2N-Y-N(CH3))-9oxothioxanthene-4-carboxaldehyde and reacting said aldehyde with pyridine hydrochloride to produce 1-(R1R2N-Y-NH)-9oxothioxanthene-4-carboxaldehyde, where R1 and R2 are each loweralkyl and Y is lower-alkylene having from two to four carbon atoms and having its two connecting linkages on different carbon atoms. The novel intermediates, 1-(R1R2N-Y-N(CH3))thioxanthen-9ones, also have antibacterial activity.
    • 通过用R1R2N-Y-NHCH3加热1-氯 - 噻吨-9-酮,制备1-(R1R2N-Y-NH)-9-氧代噻吨-4-甲醛,制备相应的4-羟甲基化合物的中间体, 得到1- [R 1 R 2 N -Y-NH(CH 3)]噻吨-9-酮,使后一化合物与磷酰卤和二甲基甲酰胺反应,得到1- [R 1 R 2 N -YN(CH 3)] - 9-氧代噻吨-4-甲醛, 所述醛与吡啶盐酸盐反应,得到1-(R1R2N-Y-NH)-9-氧代噻吨-4-甲醛,其中R 1和R 2各自为低级烷基,Y为具有2至4个碳原子的低级亚烷基, 两个不同碳原子上的连接键。 新型中间体1- [R1R2N-Y-N(CH3)]噻吨-9-酮也具有抗菌活性。