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The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: [chemical expression included] which exhibits Acetyl-CoA carboxylase (“ACC”) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

Titel:	Processes for preparing ACC inhibitors and solid forms thereof
Autor/in / Beteiligte Person:	Gilead Sciences, Inc.
Link:	View record in USPTO Patent Grants (Volltext)
Veröffentlichung:	2019
Medientyp:	Patent
Sonstiges:	Nachgewiesen in: USPTO Patent Grants Sprachen: English Patent Number: 10519,165 Publication Date: December 31, 2019 Appl. No: 15/910744 Application Filed: March 02, 2018 Assignees: Gilead Sciences, Inc. (Foster City, CA, US) Claim: 1. A method for preparing compound of formula (J): [chemical expression included] comprising the steps of: (a) contacting a compound of formula (R): [chemical expression included] with a compound of formula (S): [chemical expression included] under conditions sufficient to form a compound of formula (P): [chemical expression included] or a solvate or a hydrate thereof, (b) contacting a compound of formula (P), or a solvate or a hydrate thereof, with a base under conditions sufficient to form a compound of formula (O): [chemical expression included] or a salt, a solvate, or a hydrate thereof, (c) contacting a compound of formula (O), or a salt, a solvate, or a hydrate thereof, with a reductant and a catalyst under conditions sufficient to form a compound of formula (N): [chemical expression included] (d) contacting a compound of formula (N) with a compound of formula (M): [chemical expression included] under conditions sufficient to form a compound of formula (L): [chemical expression included] (e) contacting a compound of formula (L) with a reductant under conditions sufficient to form a compound of formula (K): [chemical expression included] and (f) contacting a compound of formula (K) with a reductant under conditions sufficient to form a compound of formula (J); wherein R 4 is C 1-3 alkyl and each R 5 is independently an optionally substituted C 1-6 alkyl or an optionally substituted C 1-6 aryl. Claim: 2. A method for preparing compound of formula (J): [chemical expression included] comprising the steps of: (a) contacting a compound of formula (R): [chemical expression included] with a compound of formula (S): [chemical expression included] under conditions sufficient to form a compound of formula (P): [chemical expression included] or a solvate or a hydrate thereof, (b) contacting a compound of formula (P), or a solvate or a hydrate thereof, with a base under conditions sufficient to form a compound of formula (O): [chemical expression included] or a salt, a solvate, or a hydrate thereof, (c) contacting a compound of formula (O), or a salt, a solvate, or a hydrate thereof, with a reductant and a catalyst under conditions sufficient to form a compound of formula (N): [chemical expression included] (d) contacting a compound of formula (N) with a compound of formula (M): [chemical expression included] under conditions sufficient to form a compound of formula (L): [chemical expression included] and (g) contacting a compound of formula (L) with a reductant under conditions sufficient to form a compound of formula (J), wherein R 4 is C 1-3 alkyl and each R 5 is independently an optionally substituted C 1-6 alkyl or an optionally substituted C 1-6 aryl. Claim: 3. The method of claim 1 , wherein R 4 is methyl. Claim: 4. The method of claim 1 , wherein R 5 is ethyl. Patent References Cited: 8969557 March 2015 Harriman et al. ; 9453026 September 2016 Harriman et al. ; 9944655 April 2018 Harriman et al. ; 10183951 January 2019 Amedio, Jr. et al. ; 2013/0123231 May 2013 Harriman et al. ; 2019/0016732 January 2019 Bhat et al. ; WO 2017/151816 September 2017 ; WO 2018/133858 July 2018 ; WO 2018/161008 September 2018 ; WO 2019/066467 April 2019 Other References: International Search Report and Written Opinion dated Jul. 3, 2018 for PCT/US2018/020747. 15 pages. cited by applicant ; U.S. Appl. No. 16/217,935, filed Dec. 12, 2018, Alexander et al. cited by applicant ; Emerson et al, “Optical rotatory dispersion. Part XIX. A series of acids, imidazolines, amidinium chlorides, and their copper complexes, related to mandelic acid”, Journal of the Chemical Society, pp. 4887-4814 (1965). cited by applicant ; Caira, “Crystalline Polymorphism of Organic Compounds”, Topics in Current Chemistry, vol. 198, pp. 163-288 (1998). cited by applicant ; Chandramouli et al, “Review on cocrystal as an approach with newer implications in pharmaceutical field,” International Journal of Medicinal Chemistry & Analysis, vol. 2, pp. 91-100 (2012). cited by applicant Primary Examiner: Stockton, Laura L Attorney, Agent or Firm: Sheppard Mullin Richter & Hampton LLP

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Processes for preparing ACC inhibitors and solid forms thereof