Erratum: "Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes" (Bioorganic & Medicinal Chemistry Letters (2012) 22 (1464-1468))

Full text of DOI:10.1016/j.bmcl.2012.01.109

Bioorganic & Medicinal Chemistry Letters 22 (2012) 2359
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Bioorganic & Medicinal Chemistry Letters
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Erratum
Erratum to ‘‘Novel heterocyclic DPP-4 inhibitors for the treatment of type
2 diabetes’’ [Bioorg. Med. Chem. Lett. 22 (2012) 1464–1468]
a
a
a
a
a
Jon M. Sutton a, , David E. Clark , Stephen J. Dunsdon , Garry Fenton , Amanda Fillmore , Neil V. Harris ,
Chris Higgs a, Chris A. Hurley a, Sussie L. Krintel a, Robert E. MacKenzie a, Alokesh Duttaroy b, Eric Gangl b,
Wiesia Maniara b, Richard Sedrani c, Kenji Namoto c, Nils Ostermann c, Bernd Gerhartz c, Finton Sirockin c,
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Jörg Trappe c, Ulrich Hassiepen c, Daniel K. Baeschlin c,
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a Argenta Discovery 2009 Ltd, Harlow CM19 5TR, UK
b Novartis Institutes for BioMedical Research, Cambridge, MA, USA
c Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland
The publisher regrets that Scheme 2 was published incorrectly. The corrected scheme appears here.
O
3
N
EtO2C
N 5
a, b
N
6
C7N
N
O
H2N
H1
CN
7
6
O
N
O
N
c, d
e, f
N
N
HN
HN
X
Y
N
O
O
CN
CN
8
9 (X/Y = NBoc/H)
(X/Y = CH2/NHBoc)
(X/Y = CH2NBoc/H)
R1
N
R1
O
O
R2
g, h
i, j
N
HN
N
X
Y
X'
Y'
N
N
N
N
O
O
CN
CN
10
11 (X'/Y' = CH2/NH2)
12 (X'/Y' = CH2NH/H)
Scheme 2. Synthesis of 7-cyanodeazaxanthines. (a) BnNCO, Pyr, rt, 18 h, (56–100%); (b) NaOMe, DMF, 70 °C, 4 h, (89–96%); (c) MeI, K2CO3, DMF, rt, 4 h, (87–100%); (d) BBr3,
xylene, reflux, 6 h, (85–100%); (e) Br2, AcOH, 45 °C, 18 h. (68–90%); (f) Boc diamine, N-methylmorpholine, DMA, l-wave, 160 °C, 20 min, (36–86%); (g) ammonium formate,
10% Pd/C, 75 °C, 30 min, (60–90%); (h) R1Br, DIPEA, DMF, 60 °C, (25–48%); (i) R2Br, K2CO3, DMF, rt, 18 h, (75–95%); (j) TFA/DCM [1:1], rt, 1 h, (75–93%).
q DOI of original article: 10.1016/j.bmcl.2011.11.054
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Corresponding authors.
E-mail address: jon.sutton@glpg.com (J.M. Sutton).
0960-894X/$ - see front matter Crown Copyright Ó 2012 Published by Elsevier Ltd. All rights reserved.
doi:10.1016/j.bmcl.2012.01.109