422
10. Ilardi EA, Vitaku E, Njardarson JT (2014) Data-mining for sulfur and fluorine: an evaluation of pharmaceuticals to reveal opportunities for drug design and discovery. J Med Chem
57:2832–2842
11. Labeeuw O, Levoin N, Billot X, Danvy D, Calmels T, Krief S, Ligneau X, Berrebi-Bertrand
I, Robert P, Lecomte JM, Schwartz JC, Capet M (2016) Synthesis and evaluation of a
2- benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists. Bioorg Med
Chem Lett 26:5263–5266
12. Carballeira NM, Montano N, Morales C, Mooney J, Torres X, Díaz D, Sanabria-Rios DJ
(2017) 2‐Methoxylated FA display unusual antibacterial activity towards clinical isolates
of methicillin‐resistant staphylococcus aureus (CIMRSA) and escherichia coli. Lipids
52:535–548
13. Zimmermann SC, Duvall B, Tsukamoto T (2019) Recent progress in the discovery of allosteric inhibitors of kidney-type glutaminase. J Med Chem 62:46–59
14. Daugulis O, Roane J, Tran LD (2015) Bidentate, monoanionic auxiliary-directed functionalization of carbon–hydrogen bonds. Acc Chem Res 48:1053–1064
15. He J, Wasa M, Chan KSL, Shao Q, Yu JQ (2017) Palladium-catalyzed transformations of
alkyl C–H bonds. Chem Rev 117:8754–8786
16. Baudoin O (2011) Transition metal-catalyzed arylation of unactivated C(sp
3
)–H bonds. Chem
Soc Rev 40:4902–4911
17. Dastbaravardeh N, Christakakou M, Haider M, Schnürch M (2014) Recent advances in
palladium- catalyzed C(sp
3 )–H activation for the formation of carbon–carbon and carbon–
heteroatom bonds. Synthesis 46:1421–1439
18. He G, Wang B, Nack WA, Chen G (2016) Syntheses and transformations of α-amino acids
via palladium-catalyzed auxiliary-directed sp
3 C–H functionalization. Acc Chem Res
49:635–645
19. Alberico D, Scott ME, Lautens M (2007) Aryl− aryl bond formation by transition-metalcatalyzed direct arylation. Chem Rev 107:174–238
20. Wencel-Delord J, Glorius F (2013) C–H bond activation enables the rapid construction and
late-stage diversification of functional molecules. Nat Chem 5:369–375
21. Ackermann L (2014) Carboxylate-assisted ruthenium-catalyzed alkyne annulations by C–H/
Het–H bond functionalizations. Acc Chem Res 47:281–295
22. Jazzar R, Hitce J, Renaudat A, Sofack-Kreutzer J, Baudoin O (2010) Functionalization
of organic molecules by transition‐metal‐catalyzed C(sp
3
)–H activation. Chem Eur J
16:2654–2672
23. Lyons TW, Sanford MS (2010) Palladium-catalyzed ligand-directed C−H functionalization
reactions. Chem Rev 110:1147–1169
24. Bhadra S, Yamamoto H (2018) Substrate directed asymmetric reactions. Chem Rev
118:3391–3446
25. Mulzer J (1999) Basic principles of asymmetric synthesis. In: Jacobsen EN, Pfaltz A,
Yamamoto H (eds) Comprehensive asymmetric catalysis, vol 1. Springer, Berlin, pp 42–79
26. Kapdi A, Maiti D (eds) (2017) Strategies for palladium-catalyzed non-directed and directed
C bond H bond functionalization. Elsevier, Amsterdam
27. Uttry A, van Gemmeren M (2020) Direct C(sp
3 )–H activation of carboxylic acids. Synthesis
52: 479-488
28. Kao LC, Sen A (1991) Platinum(II) catalysed selective remote oxidation of unactivated C–H
bonds in aliphatic carboxylic acids. J Chem Soc Chem Commun 1242–1243
29. Dangel BD, Johnson JA, Sames D (2001) Selective functionalization of amino acids in water:
a synthetic method via catalytic C−H bond activation. J Am Chem Soc 123:8149–8150
30. Janssen M, de Vos DE (2019) Pt
II
‐catalyzed hydroxylation of terminal aliphatic C(sp
3
)−H
bonds with molecular oxygen. Chem Eur J 25:10724–10734
31. Goldshleger NF, Tyabin MB, Shilov AE, Shteinman AA (1969) Zh Fiz Khim 43:2174
32. Goldshleger NF, Eskova VV, Shilov AE, Shteinman AA (1972) Zh Fiz Khim 46:1353–1354
A. Gupta et al.
10. Ilardi EA, Vitaku E, Njardarson JT (2014) Data-mining for sulfur and fluorine: an evaluation of pharmaceuticals to reveal opportunities for drug design and discovery. J Med Chem
57:2832–2842
11. Labeeuw O, Levoin N, Billot X, Danvy D, Calmels T, Krief S, Ligneau X, Berrebi-Bertrand
I, Robert P, Lecomte JM, Schwartz JC, Capet M (2016) Synthesis and evaluation of a
2- benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists. Bioorg Med
Chem Lett 26:5263–5266
12. Carballeira NM, Montano N, Morales C, Mooney J, Torres X, Díaz D, Sanabria-Rios DJ
(2017) 2‐Methoxylated FA display unusual antibacterial activity towards clinical isolates
of methicillin‐resistant staphylococcus aureus (CIMRSA) and escherichia coli. Lipids
52:535–548
13. Zimmermann SC, Duvall B, Tsukamoto T (2019) Recent progress in the discovery of allosteric inhibitors of kidney-type glutaminase. J Med Chem 62:46–59
14. Daugulis O, Roane J, Tran LD (2015) Bidentate, monoanionic auxiliary-directed functionalization of carbon–hydrogen bonds. Acc Chem Res 48:1053–1064
15. He J, Wasa M, Chan KSL, Shao Q, Yu JQ (2017) Palladium-catalyzed transformations of
alkyl C–H bonds. Chem Rev 117:8754–8786
16. Baudoin O (2011) Transition metal-catalyzed arylation of unactivated C(sp
3
)–H bonds. Chem
Soc Rev 40:4902–4911
17. Dastbaravardeh N, Christakakou M, Haider M, Schnürch M (2014) Recent advances in
palladium- catalyzed C(sp
3 )–H activation for the formation of carbon–carbon and carbon–
heteroatom bonds. Synthesis 46:1421–1439
18. He G, Wang B, Nack WA, Chen G (2016) Syntheses and transformations of α-amino acids
via palladium-catalyzed auxiliary-directed sp
3 C–H functionalization. Acc Chem Res
49:635–645
19. Alberico D, Scott ME, Lautens M (2007) Aryl− aryl bond formation by transition-metalcatalyzed direct arylation. Chem Rev 107:174–238
20. Wencel-Delord J, Glorius F (2013) C–H bond activation enables the rapid construction and
late-stage diversification of functional molecules. Nat Chem 5:369–375
21. Ackermann L (2014) Carboxylate-assisted ruthenium-catalyzed alkyne annulations by C–H/
Het–H bond functionalizations. Acc Chem Res 47:281–295
22. Jazzar R, Hitce J, Renaudat A, Sofack-Kreutzer J, Baudoin O (2010) Functionalization
of organic molecules by transition‐metal‐catalyzed C(sp
3
)–H activation. Chem Eur J
16:2654–2672
23. Lyons TW, Sanford MS (2010) Palladium-catalyzed ligand-directed C−H functionalization
reactions. Chem Rev 110:1147–1169
24. Bhadra S, Yamamoto H (2018) Substrate directed asymmetric reactions. Chem Rev
118:3391–3446
25. Mulzer J (1999) Basic principles of asymmetric synthesis. In: Jacobsen EN, Pfaltz A,
Yamamoto H (eds) Comprehensive asymmetric catalysis, vol 1. Springer, Berlin, pp 42–79
26. Kapdi A, Maiti D (eds) (2017) Strategies for palladium-catalyzed non-directed and directed
C bond H bond functionalization. Elsevier, Amsterdam
27. Uttry A, van Gemmeren M (2020) Direct C(sp
3 )–H activation of carboxylic acids. Synthesis
52: 479-488
28. Kao LC, Sen A (1991) Platinum(II) catalysed selective remote oxidation of unactivated C–H
bonds in aliphatic carboxylic acids. J Chem Soc Chem Commun 1242–1243
29. Dangel BD, Johnson JA, Sames D (2001) Selective functionalization of amino acids in water:
a synthetic method via catalytic C−H bond activation. J Am Chem Soc 123:8149–8150
30. Janssen M, de Vos DE (2019) Pt
II
‐catalyzed hydroxylation of terminal aliphatic C(sp
3
)−H
bonds with molecular oxygen. Chem Eur J 25:10724–10734
31. Goldshleger NF, Tyabin MB, Shilov AE, Shteinman AA (1969) Zh Fiz Khim 43:2174
32. Goldshleger NF, Eskova VV, Shilov AE, Shteinman AA (1972) Zh Fiz Khim 46:1353–1354
A. Gupta et al.