Sodium borohydride → Sar-125844

HRID 633480

반응식

HRID 633480 반응식
Cl[C:2]1[N:6]2[N:7]=[C:8]([C:11]3[CH:16]=[CH:15][C:14]([F:17])=[CH:13][CH:12]=3)[CH:9]=[CH:10][C:5]2=[N:4][N:3]=1.[N:18]1([CH2:24][CH2:25][NH:26][C:27]([NH:29][C:30]2[S:31][C:32]3[CH:38]=[C:37]([SH:39])[CH:36]=[CH:35][C:33]=3[N:34]=2)=[O:28])[CH2:23][CH2:22][O:21][CH2:20][CH2:19]1.[BH4-].[Na+]>C(N(CC)CC)C>[F:17][C:14]1[CH:15]=[CH:16][C:11]([C:8]2[CH:9]=[CH:10][C:5]3[N:6]([C:2]([S:39][C:37]4[CH:36]=[CH:35][C:33]5[N:34]=[C:30]([NH:29][C:27]([NH:26][CH2:25][CH2:24][N:18]6[CH2:23][CH2:22][O:21][CH2:20][CH2:19]6)=[O:28])[S:31][C:32]=5[CH:38]=4)=[N:3][N:4]=3)[N:7]=2)=[CH:12][CH:13]=1

참가 물질

5

반응물 3

HCID 4311764Sodium borohydrideHCID 446043783-Chloro-6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazineHCID 866478761-(2-Morpholin-4-ylethyl)-3-(6-sulphanyl-1,3-benzothiazol-2-yl)urea

생성물 1

HCID 25182860Sar-125844

시약·촉매·용매 1

HCID 8471Triethylamine용매

실험 절차

The 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulphanyl}-1,3-benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea was prepared according to the method described in Example 1a, but using 240 mg of 3-chloro-6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine, 338 mg of 1-(2-morpholin-4-ylethyl)-3-(6-sulphanyl-1,3-benzothiazol-2-yl)urea, 0.14 cm3 of triethylamine and 38 mg of sodium borohydride. The crude obtained is chromatographed on a Merck cartridge (30 g of silica 15-40 μm), elution being carried out with dichloromethane. 117 mg of 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulphanyl}-1,3-benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea are thus recovered in the form of a beige solid, the characteristics of which are as follows:

후처리

  1. customThe crude obtained
  2. customis chromatographed on a Merck cartridge (30 g of silica 15-40 μm), elution
  3. custom117 mg of 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulphanyl}-1,3-benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea are thus recovered in the form of a beige solid

출처 및 근거

ORD 기록
ord-d0f7aeec14ec46d89302dcaf26cb3d20
출처 데이터셋
uspto-grants-2016_04
특허 번호
US09321777B2

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