2,3-Dihydroxybutanedioic Acid → Ritanserin

HRID 1980149

반응식

HRID 1980149 반응식
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]([C:28]2[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=2)=[C:9]2[CH2:14][CH2:13][N:12]([CH2:15][CH2:16][C:17]3[C:22](=[O:23])[N:21]4[CH:24]=[CH:25][S:26][C:20]4=[N:19][C:18]=3[CH3:27])[CH2:11][CH2:10]2)=[CH:4][CH:3]=1.[OH:35][CH:36]([CH:40]([OH:44])[C:41]([OH:43])=[O:42])[C:37]([OH:39])=[O:38]>CC(O)C>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]([C:28]2[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=2)=[C:9]2[CH2:14][CH2:13][N:12]([CH2:15][CH2:16][C:17]3[C:22](=[O:23])[N:21]4[CH:24]=[CH:25][S:26][C:20]4=[N:19][C:18]=3[CH3:27])[CH2:11][CH2:10]2)=[CH:6][CH:7]=1.[OH:35][CH:36]([CH:40]([OH:44])[C:41]([O-:43])=[O:42])[C:37]([O-:39])=[O:38]

참가 물질

5

반응물 2

HCID 8752,3-Dihydroxybutanedioic AcidHCID 5074Ritanserin

생성물 2

HCID 5074Ritanserin수율 98%HCID 38061142,3-Dihydroxybutanedioate

시약·촉매·용매 1

HCID 3776Isopropanol용매

실험 절차

A mixture of 4 parts of 6-[2-[4-[bis(4-fluorophenyl)-methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]-pyrimidin-5-one, 1.3 parts of (+)-[R-(R*,R*)]-2,3-dihydroxybutanedioic acid and 96 parts of 2-propanol was stirred and heated till all solid entered solution. The whole was cooled while stirring. The product was filtered off and dried, yielding 5.1 parts (98%) of (+)-6-[2-[4-[bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one [R-(R*,R*)]-2,3-dihydroxybutanedioate(1:1).; mp. 198.7° C. (compound 147).

후처리

  1. temperatureheated till all solid
  2. temperatureThe whole was cooled
  3. stirringwhile stirring
  4. filtrationThe product was filtered off
  5. customdried

출처 및 근거

ORD 기록
ord-44e9fbaec7d64f349d1ea253b0c88813
출처 데이터셋
uspto-grants-1984_11
특허 번호
US04485107

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