Processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds

• Main Authors: BEAT WIRZ, IDING HANS, WIRZ BEAT, SAVAGE SCOTT, HAN CHONG, REENTS REINHARD
• Format: Patent
• Language: Chinese; English
• Published: 11.12.2020
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; ENZYMOLOGY; FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE; HETEROCYCLIC COMPOUNDS; METALLURGY; MICROBIOLOGY; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; SPIRITS; VINEGAR; WINE

The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes. 本公开涉及用于制备(环戊并[d]嘧啶-4-基)哌嗪化合物的方法，且更具体地涉及用于制备(R)-4-(5-甲基-7-氧代-6,7-二氢-5H-环戊并[d]嘧啶-4-基)哌嗪及其N-保护的衍生物的方法，所述化合物可用作合成伊帕斯布(即，(S)-2-(4-氯苯基)-1-(4-((5R,7R)-7-羟基-5-甲基-6,7-二氢-5H-环戊并[d]嘧啶-4-基)哌嗪-1-基)-3-(异丙基氨基)-丙-1-酮)的中间体。本公开另外涉及作为这些方法中使用的中间体的各种化合物。