Cyclopropanesulfonyl chloride → HCID 52934781, compound

HRID 1259437Notes

Reaction equation

HRID 1259437 reaction equation
[NH2:1][C:2]1[C:7]([NH:8][C:9]2[CH:14]=[CH:13][C:12]([I:15])=[CH:11][C:10]=2[F:16])=[CH:6][C:5](=[O:17])[N:4]2[CH2:18][CH2:19][S:20][C:3]=12.[CH:21]1([S:24](Cl)(=[O:26])=[O:25])[CH2:23][CH2:22]1>N1C=CC=CC=1>[F:16][C:10]1[CH:11]=[C:12]([I:15])[CH:13]=[CH:14][C:9]=1[NH:8][C:7]1[C:2]([NH:1][S:24]([CH:21]2[CH2:23][CH2:22]2)(=[O:26])=[O:25])=[C:3]2[S:20][CH2:19][CH2:18][N:4]2[C:5](=[O:17])[CH:6]=1

Participants

4

Reactant 2

HCID 2760919Cyclopropanesulfonyl chlorideHCID 583805768-Amino-7-(2-fluoro-4-iodo-phenylamino)-2,3-dihydro-thiazolo[3,2-a]pyridin-5-one

Product 1

HCID 52934781HCID 52934781, compoundYield 20%

Reagents, catalysts & solvents 1

HCID 1049PyridineSolvent

Procedure

Using the same reaction conditions and workup as described for the preparation of Example 19A, 8-amino-7-(2-fluoro-4-iodo-phenylamino)-2,3-dihydro-thiazolo[3,2-a]pyridin-5-one (0.08 g, 0.199 mmol) in pyridine (1 mL) was reacted with cyclopropylsulfonyl chloride (33 mg, 0.238 mmol) to afford the crude product. Purification by preparative HPLC afforded 20 mg of the product (20% yield).

Workup

  1. customthe same reaction conditions and workup
  2. customto afford the crude product
  3. customPurification by preparative HPLC

Sources & evidence

ORD record
ord-214160ad663d45abac71d0645e415969
Source dataset
uspto-grants-2013_06
Patent number
US08466289B2

Reaction notes

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