Invention Grant
- Patent Title: Modified nucleoside phosphoramidites
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Application No.: US17514168Application Date: 2021-10-29
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Publication No.: US12030907B2Publication Date: 2024-07-09
- Inventor: Sergei Gryaznov , Jin Hong , Vivek Kumar Rajwanshi , Leonid Beigelman
- Applicant: Janssen BioPharma, Inc.
- Applicant Address: US CA South San Francisco
- Assignee: Janssen BioPharma, Inc.
- Current Assignee: Janssen BioPharma, Inc.
- Current Assignee Address: US CA South San Francisco
- Agency: Arnold & Porter Kaye Scholer
- Main IPC: C07H19/10
- IPC: C07H19/10 ; C07H1/00 ; C07H19/20

Abstract:
A method of making a compound represented by Formula (I):
includes a reducing step, a protecting step, and a phosphitylating step, where X is NH; Y is OCF3, —O(CR42)aCR43, —O(CR42)bOCR43, or —O(CR42)b—CR4═CR42; Z is H; B is adenine (A), guanine (G), thymine (T), cytosine (C), uracil (U), 5-methylcytosine (5-me-C), or a protected version of A, G, T, C, U, or 5-me-C; each R1 is independently C1-6 alkyl or cycloalkyl; R2 is CH2CH2CN or C1-6 alkyl; or R1 and R2 together form an optionally substituted C1-6 cycloalkyl; R3 is H or PG; PG is a protecting group; R4 is independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.
includes a reducing step, a protecting step, and a phosphitylating step, where X is NH; Y is OCF3, —O(CR42)aCR43, —O(CR42)bOCR43, or —O(CR42)b—CR4═CR42; Z is H; B is adenine (A), guanine (G), thymine (T), cytosine (C), uracil (U), 5-methylcytosine (5-me-C), or a protected version of A, G, T, C, U, or 5-me-C; each R1 is independently C1-6 alkyl or cycloalkyl; R2 is CH2CH2CN or C1-6 alkyl; or R1 and R2 together form an optionally substituted C1-6 cycloalkyl; R3 is H or PG; PG is a protecting group; R4 is independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.
Information query
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