Sulfamic Acid → 6-Arylpyrido[2,3-d]pyrimidine deriv. 42

HRID 3442

반응식

HRID 3442 반응식
[NH2:1][C:2]1[N:3]=[CH:4][C:5]2[CH:11]=[C:10]([C:12]3[C:17]([Cl:18])=[CH:16][CH:15]=[CH:14][C:13]=3[Cl:19])[C:9]([NH2:20])=[N:8][C:6]=2[N:7]=1.S(=O)(=O)(O)N.N[CH2:27][CH2:28][CH2:29][N:30]1[CH2:35][CH2:34][O:33][CH2:32][CH2:31]1>>[Cl:19][C:13]1[CH:14]=[CH:15][CH:16]=[C:17]([Cl:18])[C:12]=1[C:10]1[C:9]([NH2:20])=[N:8][C:6]2[N:7]=[C:2]([NH:1][CH2:27][CH2:28][CH2:29][N:30]3[CH2:35][CH2:34][O:33][CH2:32][CH2:31]3)[N:3]=[CH:4][C:5]=2[CH:11]=1

참가 물질

4

반응물 3

HCID 5987Sulfamic AcidHCID 61055N-(3-Aminopropyl)morpholineHCID 53281136-(2,6-Dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine

생성물 1

HCID 53281446-Arylpyrido[2,3-d]pyrimidine deriv. 42

실험 절차

A mixture of 2,7-diamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidine (4.00 g) from Example 1, sulfamic acid (2.53 g) and aminopropylmorpholine (30 mL) was reacted as in Example 53. In this instance, the crude residue was washed with hot ethyl acetate followed by diethyl ether to afford 3.95 g of the title compound 6-(2,6-dichlorophenyl)-N2 -(3-morpholin-4-yl-propyl)-pyrido[2,3-d]pyrimidine-2,7-diamine, CIMS (1% NH3 in CH4): 461=M+ +C2H5, 433=M+ +H (Base), 346, 332; mp 224°-230.5° C.

후처리

  1. customwas reacted as in Example 53
  2. washIn this instance, the crude residue was washed with hot ethyl acetate

출처 및 근거

ORD 기록
ord-f61888cd7d804b09a5851ce22ce962d0
출처 데이터셋
uspto-grants-1998_03
특허 번호
US05733913

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