专利号:EP-2647639-A1 优先权日:2012-04-06 标题:ß-boration of alkene and alkyne intermediates 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-borated compounds can be used as intermediates in the synthesis of pharmaceutically active agents such as Sitagliptin.
专利号:EP-2647640-A1 优先权日:2012-04-06 标 题:ß-boration of alkene and alkyne intermediates 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-boated compounds can be used as intermediates in the synthesis of pharmaceutically active agents such as Sitagliptin.
专利号:US-7034163-B2 优先权日:2003-09-05 标 题 :Synthesis of pyrroles 发明人:PAGENKOPF BRIAN L; YU MING 权利人:UNIV TEXAS 摘要:An improved and highly efficient method for the preparation of 2-R(R=alkyl, aryl, H) pyrroles from nitrites (RCN, R=alkyl, aryl) is described using Lewis acid activated donor-acceptor cyclopropanes to react with aliphatic, aromatic, branched, α,β-unsaturated, or otherwise functionalized nitrites in a cascade [3+2] dipolar cycloaddition, dehydration and tautomerization sequence.
专利号:US-9045573-B2 优先权日:2012-05-23 标题 :Solid-phase support for oligonucleotide synthesis and oligonucleotide synthesis method 发明人:MAETA ERI; MORI KENJIRO; MIWA KAZUYA 权利人:NITTO DENKO CORP 摘要:The present invention provides a solid-phase support for oligonucleotide synthesis for synthesizing long chain oligonucleotide, RNA oligonucleotide and modified oligonucleotide at high synthetic quantity and high purity with a low loading amount of a linker. Provided is a solid-phase support for oligonucleotide synthesis comprising a porous resin bead having a monovinyl monomer unit, a crosslinkable vinyl monomer unit and a polyethylene glycol unit and a cleavable linker loaded on its surface, n the porous resin bead having a group capable of binding to a carboxy group by a dehydration condensation reaction on its surface, the cleavable linker having a carboxy group, wherein the carboxy group of the cleavable linker is bound to the group capable of binding to a carboxy group, by a dehydration condensation reaction, andn na loading amount of the cleavable linker is 1 to 80 μmol/g relative to the weight of the porous resin bead.
专利号:US-2001053862-A1 优先权日:1998-12-22 标 题:Process for preparing arylpiperidine carbinol intermediates and derivatives 发明人:RONSEN BRUCE; UPADHYAYA SUBHASH P 摘要:A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II): n n n where X is halo, C 1 -C 10 alkoxy, C 1 -C 10 haloalkyl, or hydroxy; R 2 and R 3 are each C 1 -C 4 alkyl, and R 2 and R 3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (−)-trans configuration.
专利号:WO-0037443-A1 优先权日:1998-12-22 标 题 :Process for preparing arylpiperidine carbinol intermediates and derivatives 发明人:RONSEN BRUCE; UPADHYAYA SUBHASH P 权利人:PENTECH PHARMACEUTICALS INC 摘要:A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
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合成参考文献
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