2,3-Dihydroxybutanedioic Acid → Ritanserin

HRID 1380261

反応式

HRID 1380261 の反応式
[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]

参加物

5

反応物 2

HCID 8752,3-Dihydroxybutanedioic AcidHCID 5074Ritanserin

生成物 2

HCID 5074Ritanserin収率 98%HCID 38061142,3-Dihydroxybutanedioate

試薬・触媒・溶媒 1

HCID 3776Isopropanol溶媒

実験手順

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).

後処理

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

出典と根拠

ORDレコード
ord-5e2f2c5ff7a74b2d848972eff23be1f6
出典データセット
uspto-grants-1986_04
特許番号
US04581171

関連ノート

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