A "bottom-up" approach to process development: Application of physicochemical properties of reaction products toward the development of direct-drop processes

被引:28
作者
Chen, CK [1 ]
Singh, AK [1 ]
机构
[1] Bristol Myers Squibb Pharmaceut Res Inst, Proc Res & Dev, New Brunswick, NJ 08903 USA
关键词
D O I
10.1021/op0102114
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The "bottom-up" approach to development of direct-drop processes is a powerful, yet simple, strategy that every process chemist should consider for the development of efficient, cost-effective, and environmentally friendly processes. This approach is aided by a "parallel crystallization" technique, which allows for rapid identification of multiple solvent systems for the crystallization of the desired product using a minimal amount of material and solvent. This "bottom-up" approach is illustrated by several examples where the desired product is crystallized directly from the reaction mixture.
引用
收藏
页码:508 / 513
页数:6
相关论文
共 12 条
  • [1] Anderson N. G., 2000, PRACTICAL PROCESS RE
  • [2] Process development of 5-fluoro-3-[3-[4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl]propyl]-1H-indole dihydrochloride
    Anderson, NG
    Ary, TD
    Berg, JL
    Bernot, PJ
    Chan, YY
    Chen, CK
    Davies, ML
    DiMarco, JD
    Dennis, RD
    Deshpande, RP
    Do, HD
    Droghini, R
    Early, WA
    Gougoutas, JZ
    Grosso, JA
    Harris, JC
    Haas, OW
    Jass, PA
    Kim, DH
    Kodersha, GA
    Kotnis, AS
    LaJeunesse, J
    Lust, DA
    Madding, GD
    Modi, SP
    Moniot, JL
    Nguyen, A
    Palaniswamy, V
    Phillipson, DW
    Simpson, JH
    Thoraval, D
    Thurston, DA
    Tse, K
    Polomski, RE
    Wedding, DL
    Winter, WJ
    [J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT, 1997, 1 (04) : 300 - 310
  • [3] I DRUGS RES LTD, 2000, Patent No. 0046175
  • [4] Enantioselective synthesis of alpha-phosphono sulfonate squalene synthase inhibitors: Chiral recognition in the interactions of an alpha-phosphono sulfonate inhibitor with squalene synthase
    Lawrence, RM
    Biller, SA
    Dickson, JK
    Logan, JVH
    Magnin, DR
    Sulsky, RB
    DiMarco, JD
    Gougoutas, JZ
    Beyer, BD
    Taylor, SC
    Lan, SJ
    Ciosek, CP
    Harrity, TW
    Jolibois, KG
    Kunselman, LK
    Slusarchyk, DA
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (46) : 11668 - 11669
  • [5] MERINELLI E, 1996, TETRAHEDRON, V52, P11177
  • [6] Estimation of crystal growth kinetics using differential scanning calorimetry
    Mohan, R
    Boateng, KA
    Myerson, AS
    [J]. JOURNAL OF CRYSTAL GROWTH, 2000, 212 (3-4) : 489 - 499
  • [7] Diastereoselective reaction of a Grignard reagent with chiral imides: A practical preparation of a key intermediate in the synthesis of ifetroban sodium
    Mueller, RH
    Wang, SP
    Pansegrau, PD
    Jannotti, JQ
    Poss, MA
    Thottathil, JK
    Singh, J
    Humora, MJ
    Kissick, TP
    Boyhan, B
    [J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT, 1997, 1 (01) : 14 - 19
  • [8] Mueller RH, 1999, PROCESS CHEMISTRY IN THE PHARMACEUTICAL INDUSTRY, P37
  • [9] Assessing students' conceptual understanding of solubility equilibrium
    Raviolo, A
    [J]. JOURNAL OF CHEMICAL EDUCATION, 2001, 78 (05) : 629 - 631
  • [10] A chemoselective, acid mediated conversion of amide acetal to oxazole: The key step in the synthesis of cardiovascular drug, ifetroban sodium.
    Swaminathan, S
    Singh, AK
    Li, WS
    Venit, JJ
    Natalie, KJ
    Simpson, JH
    Weaver, RE
    Silverberg, LJ
    [J]. TETRAHEDRON LETTERS, 1998, 39 (27) : 4769 - 4772