公开(公告)号：US6140515A

公开(公告)日：2000-10-31

申请号：US153403

申请日：1998-09-15

申请人： Cheng Y. Chen ,  Lushi Tan ,  Robert D. Larsen

发明人： Cheng Y. Chen ,  Lushi Tan ,  Robert D. Larsen

IPC分类号： C07D307/60 ,  C07D307/12 ,  C07C315/00 ,  C07D307/26 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D307/60

摘要： Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.

摘要翻译： 描述了可用作环加氧酶-2（COX-2）抑制剂的3-芳基，4-芳氧基呋喃-5-酮的方法。 这些化合物可用作抗炎剂。 该方法涉及不对称合成，其包括：通过Horner-Wadsworth-Emmons反应的三取代的苯乙烯衍生物制备和随后的烯丙醇的一锅三氟甲基化; 使用Sharpless不对称二羟基化和Swern氧化制备α-羟基酮; α-羟基酮与苯氧基乙酸的酯化反应; 和所得酯的Dieckman缩合。

公开(公告)号：US6040480A

公开(公告)日：2000-03-21

申请号：US248567

申请日：1999-02-11

申请人： Michael E. Pierce ,  Cheng Y. Chen ,  Anusuya Choudhury ,  Lilian A. Radesca ,  Lushi Tan ,  Dalian Zhao

发明人： Michael E. Pierce ,  Cheng Y. Chen ,  Anusuya Choudhury ,  Lilian A. Radesca ,  Lushi Tan ,  Dalian Zhao

IPC分类号： C07D265/16 ,  A61P31/18 ,  A61P37/04 ,  C07C213/00 ,  C07C213/02 ,  C07C215/68 ,  C07C215/70 ,  C07C217/58 ,  C07C221/00 ,  C07C225/22 ,  C07D265/18 ,  C07C215/00

CPC分类号： C07D265/18 ,  C07C213/00 ,  C07C213/02 ,  C07C221/00 ,  C07C2101/02

摘要： The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

摘要翻译： 本发明提供了用于不对称合成式（Ⅵ-ⅰ）的（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的新方法 ），其可用作人类免疫缺陷病毒（HIV）逆转录酶抑制剂。

公开(公告)号：US5849936A

公开(公告)日：1998-12-15

申请号：US686261

申请日：1996-07-25

申请人： Thomas R. Hoye ,  Lushi Tan

发明人： Thomas R. Hoye ,  Lushi Tan

IPC分类号： C07D307/58

CPC分类号： C07D307/58

摘要： A method for the synthesis of bis-tetrahydrofranyl Annonaceous acetogenins, including the natural products and analogs thereof, is provided which proceeds by the Pd-mediated coupling of a bis-tetrahydrofuranyl-subunit comprising a terminal alkyne, with a (C4)-hydroxybutenolide subunit comprising a terminal vinyl iodide, followed by selective reduction of the resulting enyne.

摘要翻译： 提供了一种合成双 - 四氢ran yl Ann aceous aceous gen ins ins A it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it it 包括末端乙烯基碘，然后选择性还原所得的炔。

公开(公告)号：US5587491A

公开(公告)日：1996-12-24

申请号：US405131

申请日：1995-03-15

申请人： Thomas R. Hoye ,  Lushi Tan

发明人： Thomas R. Hoye ,  Lushi Tan

IPC分类号： C07D307/58 ,  C07D305/12

CPC分类号： C07D307/58

摘要： A method for the synthesis of bis-tetrahydrofuranyl Annonaceous acetogenins, including the natural products and analogs thereof, is provided which proceeds by the Pd-mediated coupling of a bis-tetrahydrofuranyl-subunit comprising a terminal alkyne, with a (C4)-hydroxybutenolide subunit comprising a terminal vinyl iodide, followed by selective reduction of the resulting enyne.

摘要翻译： 提供了包括天然产物和其类似物合成双 - 四氢呋喃基丙酮糖的方法，其通过Pd介导的包含末端炔的双四氢呋喃基亚基与（C4） - 羟基丁烯醇内酯亚单位的偶联 包括末端乙烯基碘，然后选择性还原所得的炔。