- CEREBLON E3 LIGASE INHIBITORS
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The present disclosure provides compounds represented by Formula I: wherein R2a, R2b, R2c, R2d, R3, R13, and Z are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are cereblon (CRBN) ubiquitination inhibitors or monofunctional synthetic intermediates that can be used to prepare PROTAC molecules. CRBN ubiquitination inhibitors and PROTAC molecules are useful for the treatment of cancer and other diseases.
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Paragraph 0604
(2021/03/05)
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- Competition of substituents for ortho direction of metalation of veratric acid
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LTMP (5 equiv) metalates randomly veratric acid (1). Under external quench conditions, the thermodynamically more stable lithium 2-lithio-3,4-dimethoxybenzoate (2) reacts with a variety of electrophiles to give versatile building units that are not easily accessible by conventional means. Under in situ quench conditions (LTMP/TMSCl), a reversal of regioselectivity is observed and 6-trimethylsilyl-3,4-dimethoxybenzoic acid (10) is formed predominantly.
- Chau, Nguyet Trang Thanh,Nguyen, Thi Huu,Castanet, Anne-Sophie,Nguyen, Kim Phi Phung,Mortier, Jacques
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p. 10552 - 10557
(2008/12/23)
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- Synthesis and biological activity of C-3' ortho dihydroxyphthalimido cephalosporins
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A series of C-3' ortho dihydroxyphthalimido cephalosporins 3~7 has been prepared by reaction of C-3' aminomethyl cephalosporin 411) with the corresponding N carboethoxyphthalimides 23 ~ 25, 37, 38. These new caphalosporins exhibit excellent in vitro Gram-negative activities, including Pseudomonas aeruginosa, excellent β-lactamases stability and pharmacokinetics equivalent or better than ceftriaxone.
- Baudart,Hennequin
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p. 1458 - 1470
(2007/10/02)
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- Directed ortho metalation of n,n-diethyl benzamides. Methodology and regiospecific synthesis of useful contiguously tri- and tetra-substituted oxygenated aromatics, phthalides and phthalic anhydrides
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Full experimental details for the directed ortho metalation approch to a variety of simple ortho-substituted N,N-diethyl benzamides (Table 1) and contiguously 1,2,3- and 1,2,3,4-substituted benzamides (Tables 2) are given. The efficient conversion of these benzamides (6, 10, 12, 13, 18, 19) into phthalides (9a-b, 16b-c, 17) and phthalic anhydrides (8,16a), compounds previously available by demanding, classical methods, is detailed. A short synthesis of iso-ochracinic acid (27) is described.
- De Silva,Reed,Billedeau,Wang,Norris,Snieckus
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p. 4863 - 4878
(2007/10/02)
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