Tadalafil → 5-(5-acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-(1-ethyl-3-azetidinyl)-2,6-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one

HRID 351941

反応式

HRID 351941 の反応式
C1N([C@@H]2O[C@@H]3COP(O)(O[C@H]3[C@H]2O)=O)[C:4]2[NH:18][C:19](N)=[N:20][C:21](=[O:22])[C:3]=2[N:2]=1.BrC1C(=O)NN=C(OCCCC2C=CC(Cl)=CC=2)C=1NC[C:33]1[CH:38]=[CH:37][CH:36]=[CH:35][N:34]=1.[Na].C[C:53]1(C)S[C@@H:56]2[C@H:58]([NH:61][C:62]([C@H:64](NC(N3C(=O)N(/N=C/C4OC=CC=4)CC3)=O)[C:65]3C=CC(O)=CC=3)=O)[C:59](=O)[N:55]2[C@H:54]1C(O)=O.C(C1N[C:105]2[C:104](=[O:107])N(C)C3=N[C@@H]4CCC[C@@H]4N3C=2N=1)CCCCC.C(C1C2[C:121](=[CH:122][C:123]([C:127]([O-])=[O:128])=CC=2)N(CC2C=CC=CC=2Cl)C=1CCC)(=O)C.BrC1C(=O)NN=C(OCCCC2C=CC(Cl)=CC=2)C=1NCC1C=NC=CC=1.O1C2C=CC(CNC3C4C(=CC=C(Cl)C=4)N=C(N4CCC(C(O)=O)CC4)N=3)=CC=2OC1.CN1C(=O)[C@H]2CC3C4C(=CC=CC=4)NC=3[C@@H](C3C=CC4OCOC=4C=3)N2C(=O)C1.CN1C2=N[C@@H]3CCC[C@@H]3N2C2N=C(CC3C=CC(C(F)(F)F)=CC=3)NC=2C1=O>>[C:104]([C:36]1[CH:37]=[C:38]([C:19]2[NH:20][C:21](=[O:22])[C:3]3[C:4](=[C:62]([CH2:64][CH3:65])[N:61]([CH:58]4[CH2:59][N:55]([CH2:54][CH3:53])[CH2:56]4)[N:2]=3)[N:18]=2)[C:33]([O:128][CH2:127][CH2:123][CH2:122][CH3:121])=[N:34][CH:35]=1)(=[O:107])[CH3:105]

参加物

11

反応物 10

HCID 110635TadalafilHCID 53114861-(6-Chloro-4-(3,4-methylenedioxybenzyl)aminoquinazolin-2-yl)piperidine-4-carboxylic acidHCID 5360545Sodium2 回HCID 9571079FuzlocillinHCID 9803788ParogrelilHCID 9818343CID 9818343HCID 15473392Sch-51866HCID 222774663-Acetyl-1-(2-chlorobenzyl)-2-propylindole-6-carboxylate2 回HCID 222775034-bromo-5-(pyridylmethylamino)-6-[3-(4-chlorophenyl)-propoxy]-3(2H)pyridazinoneHCID 178418274HCID 178418274、化合物

生成物 1

HCID 1355155655-(5-acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-(1-ethyl-3-azetidinyl)-2,6-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one

実験手順

Still other type cGMP PDE5 inhibitors useful in conjunction with the present invention include:4-bromo-5-(pyridylmethylamino)-6-[3-(4-chlorophenyl)-propoxy]-3(2H)pyridazinone; 1-[4-[(1,3-benzodioxol-5-ylmethyl)amiono]-6-chloro-2-quinozolinyl]-4-piperidine-carboxylic acid, monosodium salt; (+)-cis-5,6a,7,9,9,9a-hexahydro-2-[4-(trifluoromethyl)-phenylmethyl-5-methyl-cyclopent-4,5]imidazo[2,1-b]purin-4(3H)one; furazlocillin; cis-2-hexyl-5-methyl-3,4,5,6a,7,8,9,9a-octahydrocyclopent[4,5]-imidazo[2,1-b]purin-4-one; 3-acetyl-1-(2-chlorobenzyl)-2-propylindole-6-carboxylate; 3-acetyl-1-(2-chlorobenzyl)-2-propylindole-6-carboxylate; 4-bromo-5-(3-pyridylmethylamino)-6-(3-(4-chlorophenyl) propoxy)-3-(2H)pyridazinone; I-methyl-5(5-morpholinoacetyl-2-n-propoxyphenyl)-3-n-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one; 1-[4-[(1,3-benzodioxol-5-ylmethyl)arnino]-6-chloro-2-quinazolinyl]-4-piperidinecarboxylic acid, monosodium salt; Pharmaprojects No. 4516 (Glaxo Wellcome); Pharmaprojects No. 5051 (Bayer); Pharmaprojects No. 5064 (Kyowa Hakko; see WO 96/26940); Pharmaprojects No. 5069 (Schering Plough); GF-196960 (Glaxo Wellcome); E-8010 and E-4010 (Eisai); Bay-38-3045 & 38-9456 (Bayer) and Sch-51866.

出典と根拠

ORDレコード
ord-c000eec7092c4ad5b43cc8c18cc3b3ad
出典データセット
uspto-grants-2004_06
特許番号
US06743799B2

関連ノート

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