-
1
-
-
71049126548
-
-
3 saturation and the probability of clinical success, see
-
3 saturation and the probability of clinical success, see: Lovering F., Bikker J., Humblet C. J. Med. Chem.: 2009; 52 6752
-
(2009)
J. Med. Chem.
, vol.52
, pp. 6752
-
-
Lovering, F.1
Bikker, J.2
Humblet, C.3
-
8
-
-
79952359845
-
-
Ohwada J., Ebiike H., Kawada H., Tsukazaki M., Nakamura M., Miyazaki T., Morikami K., Yoshinari K., Yoshida M., Kondoh O., Kuramoto S., Ogawa K., Aoki Y., Shimma N. Bioorg. Med. Chem. Lett.: 2011; 21 1767
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1767
-
-
Ohwada, J.1
Ebiike, H.2
Kawada, H.3
Tsukazaki, M.4
Nakamura, M.5
Miyazaki, T.6
Morikami, K.7
Yoshinari, K.8
Yoshida, M.9
Kondoh, O.10
Kuramoto, S.11
Ogawa, K.12
Aoki, Y.13
Shimma, N.14
-
9
-
-
33644798693
-
-
Choi H.-S, Wang Z., Richmond W., He X., Yang K., Jiang T., Sim T., Karanewsky D., Gu X.-J, Zhou V., Liu Y., Ohmori O., Caldwell J., Gray N., He Y. Bioorg. Med. Chem. Lett.: 2006; 16 2173
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 2173
-
-
Choi, H.-S.1
Wang, Z.2
Richmond, W.3
He, X.4
Yang, K.5
Jiang, T.6
Sim, T.7
Karanewsky, D.8
Gu, X.-J.9
Zhou, V.10
Liu, Y.11
Ohmori, O.12
Caldwell, J.13
Gray, N.14
He, Y.15
-
10
-
-
69949119703
-
-
Nagashima S., Hondo T., Nagata H., Ogiyama T., Maeda J., Hoshii H., Kontani T., Kuromitsu S., Ohga K., Orita M., Ohno K., Moritomo A., Shiozuka K., Furutani M., Takeuchi M., Ohta M., Tsukamoto S. Bioorg. Med. Chem. Lett.: 2009; 17 6926
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 6926
-
-
Nagashima, S.1
Hondo, T.2
Nagata, H.3
Ogiyama, T.4
Maeda, J.5
Hoshii, H.6
Kontani, T.7
Kuromitsu, S.8
Ohga, K.9
Orita, M.10
Ohno, K.11
Moritomo, A.12
Shiozuka, K.13
Furutani, M.14
Takeuchi, M.15
Ohta, M.16
Tsukamoto, S.17
-
11
-
-
47649108367
-
-
Sabbatini F. M., Di Fabio R., St-Denis Y., Capelli A.-M, Castiglioni E., Contini S., Donati D., Fazzolari E., Gentile G., Micheli F., Pavone F., Rinaldi M., Pasquarello A., Zampori M. G., Felice P. D., Zarantonello P., Arban R., Perini B., Vitulli G., Benedetti R., Oliosi B., Worby A. ChemMedChem: 2008; 3 226
-
(2008)
ChemMedChem
, vol.3
, pp. 226
-
-
Sabbatini, F.M.1
Di Fabio, R.2
St-Denis, Y.3
Capelli, A.-M.4
Castiglioni, E.5
Contini, S.6
Donati, D.7
Fazzolari, E.8
Gentile, G.9
Micheli, F.10
Pavone, F.11
Rinaldi, M.12
Pasquarello, A.13
Zampori, M.G.14
Felice, P.D.15
Zarantonello, P.16
Arban, R.17
Perini, B.18
Vitulli, G.19
Benedetti, R.20
Oliosi, B.21
Worby, A.22
more..
-
20
-
-
80052577435
-
-
For a recent application, including a comparison with N-protected aziridines, see
-
For a recent application, including a comparison with N-protected aziridines, see: Hebeisen P., Weiss U., Alker A., Staempfli A. Tetrahedron Lett.: 2011; 52 5229
-
(2011)
Tetrahedron Lett.
, vol.52
, pp. 5229
-
-
Hebeisen, P.1
Weiss, U.2
Alker, A.3
Staempfli, A.4
-
21
-
-
53249113781
-
-
Piller F. M., Appukkuttan P., Gavryushin A., Helm M., Knochel P. Angew. Chem. Int. Ed.: 2008; 47 6802
-
(2008)
Angew. Chem. Int. Ed.
, vol.47
, pp. 6802
-
-
Piller, F.M.1
Appukkuttan, P.2
Gavryushin, A.3
Helm, M.4
Knochel, P.5
-
22
-
-
0034725741
-
-
references therein
-
Abarbri M., Thibonnet J., Bérillon L., Dehmel F., Rottländer M., Knochel P. J. Org. Chem.: 2000; 65 4618; and references therein
-
(2000)
J. Org. Chem.
, vol.65
, pp. 4618
-
-
Abarbri, M.1
Thibonnet, J.2
Bérillon, L.3
Dehmel, F.4
Rottländer, M.5
Knochel, P.6
-
25
-
-
0025010906
-
-
Wada A., Yamamoto J., Hamaoka Y., Okhi K., Nagai S., Kanatomo S. J. Heterocycl. Chem.: 1990; 27 1831
-
(1990)
J. Heterocycl. Chem.
, vol.27
, pp. 1831
-
-
Wada, A.1
Yamamoto, J.2
Hamaoka, Y.3
Okhi, K.4
Nagai, S.5
Kanatomo, S.6
-
31
-
-
72049122384
-
-
Generally, activation by strong Lewis acids or formation of the azetidinium ion is necessary
-
Generally, activation by strong Lewis acids or formation of the azetidinium ion is necessary: Couty F., Evano G. Synlett: 2009; 3053
-
(2009)
Synlett
, pp. 3053
-
-
Couty, F.1
Evano, G.2
-
32
-
-
85041493379
-
-
Representative Procedure for the Synthesis of Azaindoline 12: To an oven-dried three-necked flask containing 4,6-dichloro-2-(thiomethyl)pyrimidine (1; 390 mg, 2.0 mmol) in anhyd THF (7.5 mL) was added TMPMgClLiCl (1 M in THF, 2.4 mL, 2.4 mmol) at r.t. After stirring for 30 min, tert-butyl (4 S)-4-methyl-1,2,3-oxathiazolidine-3-carboxylate 2,2-dioxide (5; 498 mg, 2.10 mmol) was added and the reaction was stirred for a further 1 h at r.t. 1 N Citric acid (7.5 mL) and EtOAc (7.5 mL) were added, and the reaction was stirred vigorously for 5 min before separation of the layers. The organic layer was concentrated, then the residue was stirred in TFA (5 mL) for 15 min before again being concentrated
-
3ClS: 216.03567; found: 216.03557
-
-
-
|