Chloroquine → Dapsone

HRID 443615

反応式

HRID 443615 の反応式
C1C(C2CC(=O)C3C([C:16]4[CH:17]=[C:18](Cl)[CH:19]=[CH:20][C:21]=4[N:22](O)C=3C2)=O)=CC=C(C(F)(F)F)C=1.CO[C:31]1[CH:32]=[CH:33][C:34]2[N:40]=CC=C([C@@H](O)[C@H]3N4C[C@H](C=C)[C@@H](CC4)C3)[C:35]=2[CH:36]=1.CCN(CCCC(NC1C=CN=C2C=C(Cl)C=CC=12)C)CC.C1C=C(C(F)(F)F)C2C(=C(C(O)C3NCCCC3)C=C(C(F)(F)F)N=2)C=1.CC(NC1C2N=CC=CC=2C=C(OC)C=1)CCCN.CCC1N=C(N)N=C(N)C=1C1C=CC(Cl)=CC=1.CC1(C)N(C2C=CC(Cl)=CC=2)C(N)=NC(N)=N1.COC1C(N[S:165](C2C=CC(N)=CC=2)(=[O:167])=[O:166])=NC=NC=1OC>>[CH:35]1[C:34]([NH2:40])=[CH:33][CH:32]=[C:31]([S:165]([C:18]2[CH:19]=[CH:20][C:21]([NH2:22])=[CH:16][CH:17]=2)(=[O:167])=[O:166])[CH:36]=1

参加物

9

反応物 8

HCID 2719ChloroquineHCID 4046MefloquineHCID 4908PrimaquineHCID 4993PyrimethamineHCID 9049CycloguanilHCID 17134SulfadoxineHCID 68708FloxacrineHCID 3034034Quinine

生成物 1

HCID 2955Dapsone

実験手順

Depending on the type of the second antimalarial used with the tetrahydroacridones, the preferred proportions by weight used vary. When using Floxacrine in admixture with Quinine, a ratio of 1:10 to 1:160, in particular from 1:40 to 1:80; in admixture with Chloroquine from 4:1 to 1:20, in particular 2:1 to 1:8; in admixture with Mefloquine from 1:1.25 to 1:10; in admixture with Primaquine from 1:1.25 to 1:20, in particular 1:2.5 to 1:20; in admixture with Pyrimethamine from 21:1 to 1:1.5, in particular 10.4:1 to 1:1.5; in admixture with Cycloguanil from 1:35 to 1:284, in particular 1:142 to 1:284; in admixture with Trimethroprim from 1:10 to 1:80, in particular 1:40 to 1:80; in admixture with Sulfadoxine from 1:1 L to 1:32, in particular 1:1 to 1:6; in admixture with Dapsone from 1:5 to 1:80, in particular 1:10 to 1:80, the best synergistic was obtained.

出典と根拠

ORDレコード
ord-78ac1e2c50ee4908849a4dac61fa7556
出典データセット
uspto-grants-1981_04
特許番号
US04260615

関連ノート

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