Intermediates for pyridyloxy compounds having utility as anti-peptic
申请人:Fujirebio Kabushiki Kaisha
公开号:US04977267A1
公开(公告)日:1990-12-11
The compounds of the formulas (VI) and (VII) are useful intermediates in producing pyridyloxy derivatives of the formula (I), such as, for instance, N-4-[4-(piperidinomethyl)pyridyl-2-oxy]-2-butenyl}-2-(furfurylt hio)acetamide, which are useful as anti-peptic ulcer agents. The compounds of formula (VI) have the formula ##STR1## wherein A represents a formyl group, a protected formyl group, a hydroxymethyl group or a protected hydroxymethyl group. The compounds of formula (VIII) have the formula ##STR2## wherein G represents a formyl group, a protected formyl group, a hydroxymethyl group, a hydroxymethyl group in which the hydroxyl group is protected, or a halogenomethyl group, Y represents --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, and n is 0, 1 or 2.
4-aminomethyl-pyridyl-2-oxy derivatives having anti-ulcer activity
申请人:Fujirebio Kabushiki Kaisha
公开号:US04912101A1
公开(公告)日:1990-03-27
A compound represented by the following formula or a salt thereof ##STR1## wherein each of R.sub.1 and R.sub.2 represents a lower alkyl group, or R.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, may form a substituted or unsubstituted, saturated or partially unsaturated 4- to 8-membered heterocyclic group which may contain a hetero atom selected from N, O and S, Y represents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, and n is 0, 1 or 2. This compound is useful as anti-peptic ulcer agent.
SNAr or Sulfonylation? Chemoselective Amination of Halo(het)arene Sulfonyl Halides for Synthetic Applications and Ultralarge Compound Library Design
作者:Vasyl Naumchyk、Vladyslav A. Andriashvili、Dmytro S. Radchenko、Dmytro Dudenko、Yurii S. Moroz、Andrey A. Tolmachev、Serhii Zhersh、Oleksandr O. Grygorenko
DOI:10.1021/acs.joc.3c02636
日期:2024.3.1
The chemoselectivity of halo(het)arene sulfonyl halide aminations is studied thoroughly under parallel synthesis conditions, and the scope and limitations of the method are established. It is shown that SNAr-reactive sulfonyl halides typically undergo sulfonamide synthesis during the first step; the second amination is also possible provided that the SNAr-active center is sufficiently reactive. On
在平行合成条件下深入研究了卤代(杂)芳烃磺酰卤胺化物的化学选择性,并确定了该方法的范围和局限性。结果表明, SN Ar反应性磺酰卤通常在第一步中进行磺酰胺合成;如果SN Ar活性中心具有足够的反应性,则第二次胺化也是可能的。相反,带有芳基化部分的磺酰氟在适当的控制下在后一个反应中心发生选择性转化。进一步的硫-氟化物交换(SuFEx)也是可能的,这对于某些磺酰卤类特别有价值。开发的两步并行双胺化方案提供了对 66.7 亿个化合物的合成可处理 REAL 型化学空间的访问(预期合成成功率 76%)。
The Reaction of Sodium Azide with Some Representative Epoxides
作者:Calvin A. Vander Werf、Robert V. Heisler、William E. McEwen
DOI:10.1021/ja01634a008
日期:1954.3
Marszak-Fleury,A.; Laroche,J., Bulletin de la Societe Chimique de France, 1963, p. 1270 - 1272