Hydrochloric Acid → 2-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl L-lysyl-L-alaninate dihydrochloride

HRID 1968339노트

반응식

HRID 1968339 반응식
C(OC([NH:8][C@H:9]([C:22]([NH:24][C@H:25]([C:27]([O:29][CH2:30][CH2:31][O:32][C:33]1[CH:38]=[CH:37][C:36]([C:39]2[C:44]([C:45]#[N:46])=[C:43]([N:47]3[CH2:51][CH2:50][CH2:49][CH2:48]3)[N:42]=[C:41]([S:52][CH2:53][C:54]3[N:55]=[C:56]([C:59]4[CH:64]=[CH:63][C:62]([Cl:65])=[CH:61][CH:60]=4)[S:57][CH:58]=3)[C:40]=2[C:66]#[N:67])=[CH:35][CH:34]=1)=[O:28])[CH3:26])=[O:23])[CH2:10][CH2:11][CH2:12][CH2:13][NH:14]C(OC(C)(C)C)=O)=O)(C)(C)C.[ClH:68]>ClCCl.C(OCC)C>[ClH:65].[ClH:68].[NH2:8][C@H:9]([C:22]([NH:24][C@H:25]([C:27]([O:29][CH2:30][CH2:31][O:32][C:33]1[CH:34]=[CH:35][C:36]([C:39]2[C:44]([C:45]#[N:46])=[C:43]([N:47]3[CH2:48][CH2:49][CH2:50][CH2:51]3)[N:42]=[C:41]([S:52][CH2:53][C:54]3[N:55]=[C:56]([C:59]4[CH:64]=[CH:63][C:62]([Cl:65])=[CH:61][CH:60]=4)[S:57][CH:58]=3)[C:40]=2[C:66]#[N:67])=[CH:37][CH:38]=1)=[O:28])[CH3:26])=[O:23])[CH2:10][CH2:11][CH2:12][CH2:13][NH2:14]

참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 866438502-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl N2,N6-bis(tert-butoxycarbonyl)-L-lysyl-L-alaninate

생성물 1

HCID 687649662-{4-(2-({(2-(4-Chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl L-lysyl-L-alaninate dihydrochloride

시약·촉매·용매 2

HCID 3283Diethyl Ether용매HCID 6344Dichloromethane용매

실험 절차

300 mg (0.308 mmol) of 2-{4-(2-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl N2,N6-bis(tert-butoxycarbonyl)-L-lysyl-L-alaninate (Example 26A) were initially charged in 5.4 ml of dichloromethane. 3.08 ml (6.163 mmol) of a 1N solution of hydrogen chloride in diethyl ether were added, and the reaction solution was then stirred at RT overnight. The solid formed was filtered off, triturated with 2.5 ml of cold dichloromethane and filtered off again. This gave 250 mg (96% of theory) of the target compound.

후처리

  1. customThe solid formed
  2. filtrationwas filtered off
  3. customtriturated with 2.5 ml of cold dichloromethane
  4. filtrationfiltered off again

출처 및 근거

ORD 기록
ord-e1f1e8ec777f444c90b3bbb0faddc0d5
출처 데이터셋
uspto-grants-2013_04
특허 번호
US08420825B2

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