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Hydrochloric Acid → (S)-1-((S)-4-((2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-3-methylpiperazin-1-yl)-2-hydroxypropan-1-one

HRID 390907
ノート
印刷プレビュー

反応式

HRID 390907 の反応式
ClC1[N:3]=[C:4]([N:13]2[CH2:18][CH2:17]OCC2)[C:5]2SC(C=O)=C[C:6]=2N=1.C(N1CCN[C@@H](C)C1)(C1C=CC=CC=1)(C1C=CC=CC=1)C1C=CC=CC=1.Cl.[OH-].[Na+].C[C@H]1CNCCN1CC1N=C(N2CCOCC2)C2SC=CC=2N=1.C(O)(=O)C(C)O.Cl[C:78]1[N:79]=[C:80]([N:100]2[CH2:105][CH2:104][O:103][CH2:102][CH2:101]2)[C:81]2[S:86][C:85]([CH2:87][N:88]3[CH2:93][CH2:92][N:91]([C:94](=[O:98])[C@@H:95]([OH:97])[CH3:96])[CH2:90][C@@H:89]3[CH3:99])=[CH:84][C:82]=2[N:83]=1.CC1(C)C(C)(C)OB(C2C=CC(N)=NC=2)O1>CO>[NH2:3][C:4]1[N:13]=[CH:18][C:17]([C:78]2[N:79]=[C:80]([N:100]3[CH2:105][CH2:104][O:103][CH2:102][CH2:101]3)[C:81]3[S:86][C:85]([CH2:87][N:88]4[CH2:93][CH2:92][N:91]([C:94](=[O:98])[C@@H:95]([OH:97])[CH3:96])[CH2:90][C@@H:89]4[CH3:99])=[CH:84][C:82]=3[N:83]=2)=[CH:6][CH:5]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

10

反応物 8

HCID 313Hydrochloric AcidHCID 612Lactic AcidHCID 14798Sodium HydroxideHCID 27565555-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amineHCID 7171814(S)-4-N-Trityl-2-methyl-piperazineHCID 457899852-Chloro-4-morpholinothieno[3,2-d]pyrimidine-6-carbaldehyde
HCID 86623524
(S)-1-((S)-4-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-3-methylpiperazin-1-yl)-2-hydroxypropan-1-one
HCID 131728701((S)-2-methylpiperazin-1-yl)methyl-4-morpholinothieno[3,2-d]pyrimidine

生成物 1

HCID 58233889(S)-1-((S)-4-((2-(6-aminopyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-3-methylpiperazin-1-yl)-2-hydroxypropan-1-one収率 14.4%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

2-Chloro-4-morpholinothieno[3,2-d]pyrimidine-6-carbaldehyde 10 from Example 3 (200 mg) was used according to General Procedure B-3 with (S)-4-N-trityl-2-methyl-piperazine. The crude product was then dissolved in 10 mL of methanol and reacted with 0.5 mL of concentrated HCl for several hours before basifying with NaOH and extracting into EtOAc. After evaporation the crude reaction mixture containing 200 mg of 2-chloro-6-(((S)-2-methylpiperazin-1-yl)methyl-4-morpholinothieno[3,2-d]pyrimidine was reacted with lactic acid via General Procedure B-2. 120 mg of (S)-1-((S)-4-((2-chloro-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)-3-methylpiperazin-1-yl)-2-hydroxypropan-1-one was reacted with 88 mg of 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine via General Procedure A to give 19.6 mg of 193. MS (Q1) 498.3 (M)+.

後処理

  1. extractionextracting into EtOAc
  2. customAfter evaporation the crude
  3. customreaction mixture

出典と根拠

ORDレコード
ord-74ec09d88c604c4395f80d33979a547a
出典データセット
uspto-grants-2013_02
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08383620B2

反応ノート

読み込み中…

このページの内容参加物実験手順後処理出典と根拠反応ノート