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PROCESO PARA PREPARAR OLIGÓMEROS DE MORFOLINO FOSFORODIAMIDATO
专利权人:
SAREPTA THERAPEUTICS; INC.
发明人:
申请号:
ARP170101417
公开号:
AR108590A1
申请日:
2017.05.24
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
In the present processes are provided for preparing an oligomer (For example, a morpholino oligomer).The Synthetic processes described in this can be advantageous to increase the oligomeros\u00edntesis while keeping the overall yield and Purity Of synthesized oligomer.Claim 1, a process for preparing an oligomeric Compound of formula (1), where n is an integer from 10 to 40, and each R\u00b2 is selected independently for each occurrence.The Group consists of: the Group compounds of formulas (2),Where the process involves the Sequential steps of: (a) contacting a compound of formula (3), where r\u00b9 is a means of support and r\u00b3 is selected from the group consisting tritilo,Monometoxitritilo,Dimetoxitritilo and trimetoxitritilo with release Agent to form the compound of formula (4), where r\u00b9 is a means of support (b) contacting the compound of formula (4) with a CComprised of formula (5), where r\u00b3 is selected from the group consisting tritilo, monometoxitritilo,Dimetoxitritilo and trimetoxitritilo to form a compound of formula (6), where r\u00b9 is a means of support, and r\u00b3 is selected from the group consisting tritilo, monometoxitritilo,Dimetoxitritilo and trimetoxitritilo (c) contacting the compound of formula (6) with a release Agent to form a compound of formula (7), where r\u00b9 is a means of support (d)R in the compound of formula (7) with a compound of formula (8) where r\u00b3 is selected from the group consisting tritilo, monometoxitritilo, dimetoxitritilo and trimetoxitritilo,And r\u2074 is selected from the group consisting of: the Group compounds of Formulae (9) to form a compound of formula (10) where r\u00b9 is a support MediumR\u00b3 is selected from the group consisting tritilo, monometoxitritilo, dimetoxitritilo and trimetoxitritilo,And r\u2074 is selected: group compounds of Formulae (9) (e) n-1 iterations of the Sequential steps of: (a) contacting the product formed by the step immediately previOr with a release Agent (E2) an
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