Tert-Butylamine → Boc-Hyp-NH-tBu

HRID 2269649ノート

反応式

HRID 2269649 の反応式
[C:1]([N:8]1[CH2:16][C@H:14]([OH:15])[CH2:13][C@H:9]1[C:10]([OH:12])=O)([O:3][C:4]([CH3:7])([CH3:6])[CH3:5])=[O:2].[C:17]([NH2:21])([CH3:20])([CH3:19])[CH3:18].C1C=CC2N(O)N=NC=2C=1.CCN=C=NCCCN(C)C.Cl>ClCCl>[N:8]1([C:1]([O:3][C:4]([CH3:5])([CH3:6])[CH3:7])=[O:2])[CH2:16][C@H:14]([OH:15])[CH2:13][C@H:9]1[C:10]([NH:21][C:17]([CH3:20])([CH3:19])[CH3:18])=[O:12]

参加物

6

反応物 4

HCID 6385Tert-ButylamineHCID 757711-HydroxybenzotriazoleHCID 88804(2S,4R)-4-hydroxy-1-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidine-2-carboxylic acidHCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride

生成物 1

HCID 10334194Boc-Hyp-NH-tBu収率 189%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

In a dichloromethane solution containing 5.1 g of N-Boc-hydroxyproline (Boc-Hyp-OH), 0.35 g of tert-butylamine, 7.4 g of HOBt and 6.0 g of EDC hydrochloride were added under ice cooling and the resultant mixture was stirred overnight at room temperature. The reaction mixture was treated similarly to that in Example 144 (Process 2) to give 2.59 g of the title compound.

後処理

  1. additionwere added under ice cooling
  2. additionThe reaction mixture was treated similarly to that in Example 144 (Process 2)

出典と根拠

ORDレコード
ord-16f3afdf35f64f9ebb9c807e7d6e60f0
出典データセット
uspto-grants-2001_12
特許番号
US06329502B1

反応ノート

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