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Process methods for inhibitors of phosphatidylinositol 3-kinase
专利权人:
GILEAD CALISTOGA LLC
发明人:
申请号:
ARP140104806
公开号:
AR098871A1
申请日:
2014.12.19
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
At present, there is a process for the synthesis of compounds containing quinine that may help to treat cancer. In addition, intermediate compounds related to these processes are also disclosed. Claim 1: a process for synthesizing a formula (1) or a salt compound thereof, including a stage (a), wherein a compound of formula (2) or a salt thereof is combined with a compound of formula (3),wherein the compound of the formula (1) or one of its salts is synthesized, wherein R¹ is halo; R² is selected from the group consisting of H and optionally substituted C₁₋₈ alkyl; and R³ and R⁴ are each independently selected from the group consisting of hydrogen, an amino protecting group and an optionally substituted purinyl group. Claim 2: The process according to claim 1, which also comprises step b) of combining the compound of the formula (1) or one of its salts; and a compound of the formula (9) wherein n is 0-5; and each R⁵ is independently selected from the group consisting of alkyl, alkenyl,Pitch, anthrax, anthrax, aminobenzene, hydroxy, halogen, cf-83323;1. Amino, amine replaced, nitro, tiol, Ciano, cyclo, cyclo, heatcycle, arilo and heateral; it synthesized a formula compound (4) or a salt. 3. Claim 3: the process described in claim 2 also includes (c) a combined formula (4) compound or a salt thereof, wherein at least one formula (4) compound containing R 3 and r83088 is an ammonia protection group; and one or more reactants, 1. One or more reagents are used to remove Amin protection group; it synthesizes a formula (5) or a salt thereof;(d) A compound combining formula (5) or its salts and formula (6),a. X was selected from halogen, Messiah, methylacetic acid, thyroid and thyroid groups; r8310 was hydrogen or amino protected group; it synthesized a formula compound (7) or its salts; r8310 was an ammonia protected group; (e) The stage also includes one (7) formulation compound or one of its salts; and one or more reagents, one or more of which are used to remove the amm
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