Hydrochloric Acid → 9-((1R,2S,3R,4S)-4-Amino-2,3-dihydroxy-cyclopentyl)-6-(2,2-diphenyl-ethylamino)-9H-purine-2-carboxylic acid (2-{3-[1-(3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-ylcarbamoyl)-piperidin-4-yl]-ureido}-ethyl)-amide dihydrochloride

HRID 2382437Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2382437
C(OC(=O)[NH:7][C@H:8]1[CH2:12][C@@H:11]([N:13]2[CH:21]=[N:20][C:19]3[C:14]2=[N:15][C:16]([C:37](=[O:66])[NH:38][CH2:39][CH2:40][NH:41][C:42]([NH:44][CH:45]2[CH2:50][CH2:49][N:48]([C:51](=[O:65])[NH:52][CH:53]4[CH2:58][CH2:57][N:56]([C:59]5[CH:64]=[CH:63][CH:62]=[CH:61][N:60]=5)[CH2:55][CH2:54]4)[CH2:47][CH2:46]2)=[O:43])=[N:17][C:18]=3[NH:22][CH2:23][CH:24]([C:31]2[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=2)[C:25]2[CH:30]=[CH:29][CH:28]=[CH:27][CH:26]=2)[C@H:10]([OH:67])[C@@H:9]1[OH:68])(C)(C)C.[ClH:70]>CO.O1CCOCC1>[ClH:70].[ClH:70].[N:56]1([C:59]2[CH:64]=[CH:63][CH:62]=[CH:61][N:60]=2)[CH2:57][CH2:58][CH:53]([NH:52][C:51]([N:48]2[CH2:47][CH2:46][CH:45]([NH:44][C:42](=[O:43])[NH:41][CH2:40][CH2:39][NH:38][C:37]([C:16]3[N:15]=[C:14]4[C:19]([N:20]=[CH:21][N:13]4[C@@H:11]4[CH2:12][C@H:8]([NH2:7])[C@@H:9]([OH:68])[C@H:10]4[OH:67])=[C:18]([NH:22][CH2:23][CH:24]([C:31]4[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=4)[C:25]4[CH:26]=[CH:27][CH:28]=[CH:29][CH:30]=4)[N:17]=3)=[O:66])[CH2:50][CH2:49]2)=[O:65])[CH2:54][CH2:55]1

Komponenten

5

Edukt 2

HCID 313Hydrochloric AcidHCID 86647556{(1S,2R,3S,4R)-4-[6-(2,2-Diphenyl-ethylamino)-2-(2-{3-[1-(3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-ylcarbamoyl)-piperidin-4-yl]-ureido}-ethylcarbamoyl)-purin-9-yl]-2,3-dihydroxy-cyclopentyl}-carbamic acid tert-butyl ester

Produkt 1

HCID 866475579-((1R,2S,3R,4S)-4-Amino-2,3-dihydroxy-cyclopentyl)-6-(2,2-diphenyl-ethylamino)-9H-purine-2-carboxylic acid (2-{3-[1-(3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4-ylcarbamoyl)-piperidin-4-yl]-ureido}-ethyl)-amide dihydrochloride

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 887MethanolLösungsmittelHCID 312751,4-DioxaneLösungsmittel

Versuchsvorschrift

A solution of {(1S,2R,3S,4R)-4-[6-(2,2-diphenyl-ethylamino)-2-(2-{3-[1-(3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylcarbamoyl)-piperidin-4-yl]-ureido}-ethylcarbamoyl)-purin-9-yl]-2,3-dihydroxy-cyclopentyl}-carbamic acid tert-butyl ester (76.7 mg, 81 μmol) in MeOH (0.5 ml) is treated with 4M HCl in dioxane (0.5 ml). After stirring at room temperature for 1 hour, the solvent is removed in vacuo to afford the title compound which is used crude in the next step.

Aufarbeitung

  1. customthe solvent is removed in vacuo

Quellen und Nachweise

ORD-Eintrag
ord-9f4aec223ffd4fd980838049cfa30fb2
Quelldatensatz
uspto-grants-2012_09
Patentnummer
US08258141B2

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