(-)-Mandelic acid → (2R)-2-(2-amino-2-methylpropanamido)-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide(R)-(-)-mandelate

HRID 2070164ノート

反応式

HRID 2070164 の反応式
[NH2:1][C:2]([CH3:38])([CH3:37])[C:3]([NH:5][C@H:6]([CH2:33][CH:34]([CH3:36])[CH3:35])[C:7]([NH:9][CH:10]1[CH2:19][C:18]2[C:13](=[C:14]([N:20]3[CH2:24][CH2:23][CH2:22][C:21]3=[O:25])[CH:15]=[CH:16][CH:17]=2)[N:12]([CH2:26][C:27]2[CH:31]=[CH:30][S:29][CH:28]=2)[C:11]1=[O:32])=[O:8])=[O:4].[C:39]([OH:49])(=[O:48])[C@@H:40]([C:42]1[CH:47]=[CH:46][CH:45]=[CH:44][CH:43]=1)[OH:41]>C(OCC)(=O)C>[C:39]([OH:49])(=[O:48])[C@@H:40]([C:42]1[CH:47]=[CH:46][CH:45]=[CH:44][CH:43]=1)[OH:41].[NH2:1][C:2]([CH3:37])([CH3:38])[C:3]([NH:5][C@H:6]([CH2:33][CH:34]([CH3:35])[CH3:36])[C:7]([NH:9][CH:10]1[CH2:19][C:18]2[C:13](=[C:14]([N:20]3[CH2:24][CH2:23][CH2:22][C:21]3=[O:25])[CH:15]=[CH:16][CH:17]=2)[N:12]([CH2:26][C:27]2[CH:31]=[CH:30][S:29][CH:28]=2)[C:11]1=[O:32])=[O:8])=[O:4]

参加物

4

反応物 2

HCID 11914(-)-Mandelic acidHCID 59620332(2R)-2-(2-amino-2-methylpropanamido)-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide

生成物 1

HCID 89723348(2R)-2-(2-amino-2-methylpropanamido)-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide(R)-(-)-mandelate

試薬・触媒・溶媒 1

HCID 8857Ethyl Acetate溶媒

反応条件

温度
70 °C

実験手順

(2R)-2-(2-Amino-2-methylpropanamido)-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide (542 mg) was dissolved in ethyl acetate (6.5 mL), and (R)-(−)-mandelic acid (141 mg) was added thereto. The mixture was stirred at 70° C. for 10 minutes, and then left to stand to cool to room temperature. The formed precipitates were recovered through filtration, washed with ethyl acetate, and dried under reduced pressure, whereby the title compound (589 mg) was yielded.

後処理

  1. waitleft
  2. temperatureto cool to room temperature
  3. customThe formed precipitates
  4. filtrationwere recovered through filtration
  5. washwashed with ethyl acetate
  6. dry with materialdried under reduced pressure, whereby the title compound (589 mg)
  7. customwas yielded

出典と根拠

ORDレコード
ord-6fcb5adfd5d24a6ca11f811a666a7482
出典データセット
uspto-grants-2012_10
特許番号
US08299255B2

反応ノート

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