509092-16-4Relevant academic research and scientific papers
PROCESS FOR PRODUCING 2-AMINO-2-[2-[4-(3-BENZYLOXY-PHENYLTHIO)-2-CHLOROPHENYL[ETHYL]-1,3-PROPANEDIOL HYDROCHLORIDE OR HYDRATE THEREOF AND INTERMEDIATE FOR THE SAME
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Page/Page column 9-10, (2008/06/13)
A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro
Efficient synthesis of the immunomodulating compound KRP-203
Hamada, Maiko,Kiuchi, Masatoshi,Adachi, Kunitomo
, p. 1927 - 1929 (2008/02/10)
A practical and concise synthesis of KRP-203 (1) was achieved by utilizing a palladium coupling reaction mediated by XantPhos and Pd2(dba) 3 as the key step. The coupling reaction of aryl bromide 5 with 3-hydroxythiophenol (6) proceeded chemoselectively to give phenol 7 in spite of the presence of a chlorine substituent on 5 and a hydroxyl group on 6. Phenol 7 was converted into KRP-203 by benzylation and removal of the protecting groups in high yield. Georg Thieme Verlag Stuttgart.
