Detail of "17746-05-3"

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Thiazolidine derivatives, intermediates therefor, and pharmaceutical preparations

Thiazolidine derivatives, intermediates therefor, and pharmaceutical preparations. Hasler, Heinz; Schneider, Fernand (Hoffmann-La Roche, F., und Co. A.In this study，17746-05-3 is also used.-G., Switz.). Eur. Pat. Appl. EP 129747 A2 2 Jan 1985, 25 pp. DESIGNATED STATES: R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (German). (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07D513-10. ICS: C07D277-60; A61K031-425. ICA: C07D311-22; C07D409-04. ICI: C07D513-10, C07D311-00, C07D277-00. APPLICATION: EP 84-106419 5 Jun 1984. 17746-05-3 is also in the experiment. PRIORITY: CH 83-3432 23 Jun 1983; CH 84-1860 13 Apr 1984. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 7, 63 Spirothiazolidinediones I (R = H, halo, NO2; R1 = H, NO2, cyano, R2O, R2NH; R2 = H, alkyl, acyl, R3O2C, R3NHCO; R3 = alkyl, aryl, aralkyl; X = CH2, O, S, X1 = O) were prepd. Thus, 4-FC6H4OH was alkylated with CH2:CHCN and the product hydrolyzed with aq. HCl to give 4-FC6H4OCH2CH2CO2H. This was cyclized by heating with polyphosphoric acid and the chromanone treated with BuLi and 2-(trimethylsilyl)-1,3-dithiane to give dithianylidenebenzopyran II. This was treated successively with N-chlorosuccinimide in EtOH and H2NCSNH3 to give I (R = F, R = H, X = O, X1 = NH) which was hydrolyzed in aq. HCl to give I (R = F, R1 = H, X = X1 = O) (III). III is an inhibitor of aldose reductase with an IC50 of 0.10 mM. ..

Thiazolidine derivatives, intermediates therefor, and pharmaceutical preparations

Thiazolidine derivatives, intermediates therefor, and pharmaceutical preparations. Hasler, Heinz; Schneider, Fernand (Hoffmann-La Roche, F., und Co. A.In this study，17746-05-3 is also used.-G., Switz.). Eur. Pat. Appl. EP 129747 A2 2 Jan 1985, 25 pp. DESIGNATED STATES: R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (German). (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07D513-10. ICS: C07D277-60; A61K031-425. ICA: C07D311-22; C07D409-04. ICI: C07D513-10, C07D311-00, C07D277-00. APPLICATION: EP 84-106419 5 Jun 1984. 17746-05-3 is also in the experiment. PRIORITY: CH 83-3432 23 Jun 1983; CH 84-1860 13 Apr 1984. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 7, 63 Spirothiazolidinediones I (R = H, halo, NO2; R1 = H, NO2, cyano, R2O, R2NH; R2 = H, alkyl, acyl, R3O2C, R3NHCO; R3 = alkyl, aryl, aralkyl; X = CH2, O, S, X1 = O) were prepd. Thus, 4-FC6H4OH was alkylated with CH2:CHCN and the product hydrolyzed with aq. HCl to give 4-FC6H4OCH2CH2CO2H. This was cyclized by heating with polyphosphoric acid and the chromanone treated with BuLi and 2-(trimethylsilyl)-1,3-dithiane to give dithianylidenebenzopyran II. This was treated successively with N-chlorosuccinimide in EtOH and H2NCSNH3 to give I (R = F, R = H, X = O, X1 = NH) which was hydrolyzed in aq. HCl to give I (R = F, R1 = H, X = X1 = O) (III). III is an inhibitor of aldose reductase with an IC50 of 0.10 mM. ..